1. Metabolic Enzyme/Protease Anti-infection
  2. HIV Integrase HIV
  3. Elvitegravir

Elvitegravir  (Synonyms: 埃替拉韦; GS-9137; JTK-303; D06677)

目录号: HY-14740 纯度: 99.90%
COA 产品使用指南

Elvitegravir (GS-9137; JTK-303; D06677) 是一种 HIV integrase 抑制剂,作用于 HIV-1IIIBHIV-2EHOHIV-2RODIC50 分别为 0.7 nM,2.8 nM 和 1.4 nM。

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Elvitegravir Chemical Structure

Elvitegravir Chemical Structure

CAS No. : 697761-98-1

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10 mM * 1 mL in DMSO ¥972
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5 mg ¥552
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10 mg ¥884
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50 mg ¥3464
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100 mg ¥5200
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Customer Review

Other Forms of Elvitegravir:

    Elvitegravir purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2016;38(3):1111-20.  [Abstract]

    Arithmetic means±SEM (n=10) of erythrocyte annexin-V-binding following incubation for 48 hours to Ringer solution without (white bar) or with (black bars) Elvitegravir (0.5-2.5 µg/mL).

    Elvitegravir purchased from MCE. Usage Cited in: Antimicrob Agents Chemother. 2015 Dec;59(12):7666-7670.  [Abstract]

    Effects of antiviral drugs on cellular uptake of fluorescein by BeWo cells. The cells are incubated with 1 μM fluorescein in the presence of 100 μM compounds for 10 min at 37°C.

    查看 HIV 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Elvitegravir (GS-9137; JTK-303; D06677) is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.

    IC50 & Target

    HIV-1

     

    HIV-2

     

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    C8166 EC50
    0.00021 μM
    Compound: 1
    Antiviral activity against wild type HIV1 LAI-3B infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against wild type HIV1 LAI-3B infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 21862337]
    C8166 EC50
    0.00021 μM
    Compound: Elvitegravir
    Antiviral activity against HIV1 LAI 3B infected in human C8166 cells assessed as protection against virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV1 LAI 3B infected in human C8166 cells assessed as protection against virus-induced cytopathic effect by MTT assay
    [PMID: 21763149]
    C8166 EC50
    0.001 μM
    Compound: 1
    Antiviral activity against HIV1 A17 harboring reverse transcriptase Y181C mutant infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV1 A17 harboring reverse transcriptase Y181C mutant infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 21862337]
    C8166 CC50
    17.2 μM
    Compound: 1
    Cytotoxicity against human C8166 cells by MTT assay
    Cytotoxicity against human C8166 cells by MTT assay
    [PMID: 21862337]
    C8166 CC50
    17.2 μM
    Compound: Elvitegravir
    Cytotoxicity against human C8166 cells by MTT assay
    Cytotoxicity against human C8166 cells by MTT assay
    [PMID: 21763149]
    HEK-293T CC50
    > 250 μM
    Compound: Elvitegravir
    Cytotoxicity against human HEK293T cells assessed as cell growth inhibition by MTT assay
    Cytotoxicity against human HEK293T cells assessed as cell growth inhibition by MTT assay
    [PMID: 36898139]
    HeLa CC50
    > 50 μM
    Compound: EVG
    Cytotoxicity against human HeLa-CD4-LTR-beta-gal cells after 24 hrs by ATPlite reagent based luminescence analysis
    Cytotoxicity against human HeLa-CD4-LTR-beta-gal cells after 24 hrs by ATPlite reagent based luminescence analysis
    [PMID: 25961960]
    HeLa CC50
    > 50 μM
    Compound: 1, EVG
    Cytotoxicity against human HeLa cells expressing CD4-LTR-beta-gal after 24 hrs by ATPlite assay
    Cytotoxicity against human HeLa cells expressing CD4-LTR-beta-gal after 24 hrs by ATPlite assay
    [PMID: 24684270]
    HeLa EC50
    0.0142 μM
    Compound: 1, EVG
    Antiviral activity against HIV1 3B infected in human HeLa cells expressing CD4-LTR-beta-gal assessed as inhibition of viral replication after 3 days by reporter gene assay
    Antiviral activity against HIV1 3B infected in human HeLa cells expressing CD4-LTR-beta-gal assessed as inhibition of viral replication after 3 days by reporter gene assay
    [PMID: 24684270]
    MT4 EC50
    0.00037 μM
    Compound: 2, elvitegravir, GS-9137
    Antiviral activity against HIV1 3B in MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV1 3B in MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 18665580]
    MT4 EC50
    0.0006 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 NL4.3 harboring integrase L74M mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV 1 NL4.3 harboring integrase L74M mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 18378713]
    MT4 EC50
    0.0007 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 18378713]
    MT4 EC50
    0.0008 μM
    Compound: 1, GS-9137
    Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 21227550]
    MT4 EC50
    0.0009 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 NL4.3 integrase S230N mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV 1 NL4.3 integrase S230N mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 18378713]
    MT4 EC50
    0.001 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 18378713]
    MT4 EC50
    0.0022 μM
    Compound: 3, EVG
    Antiviral activity against HIV1 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay
    Antiviral activity against HIV1 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay
    [PMID: 25907370]
    MT4 EC50
    0.0031 μM
    Compound: 3, EVG
    Antiviral activity against wild-type HIV1 3B infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay
    Antiviral activity against wild-type HIV1 3B infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay
    [PMID: 25907370]
    MT4 EC50
    0.012 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 NL4.3 integrase E92Q mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    Antiviral activity against HIV 1 NL4.3 integrase E92Q mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay
    [PMID: 18378713]
    MT4 EC50
    0.015 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound
    Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound
    [PMID: 18378713]
    MT4 EC50
    0.018 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 40 passages selected in presence of compound
    Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 40 passages selected in presence of compound
    [PMID: 18378713]
    MT4 EC50
    0.033 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 3B harboring integrase E92Q S230N double mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 20 passages in presence of compound
    Antiviral activity against HIV 1 3B harboring integrase E92Q S230N double mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 20 passages in presence of compound
    [PMID: 18378713]
    MT4 EC50
    0.05 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 3B harboring integrase L34M mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 40 passages in presence of compound
    Antiviral activity against HIV 1 3B harboring integrase L34M mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 40 passages in presence of compound
    [PMID: 18378713]
    MT4 EC50
    0.059 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 60 passages selected in presence of compound
    Antiviral activity against HIV 1 RIN HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 60 passages selected in presence of compound
    [PMID: 18378713]
    MT4 EC50
    0.077 μM
    Compound: GS-9137
    Antiviral activity against HIV 1 3B harboring integrase E92Q, S230N and L34M triple mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 60 passages in presence of compound
    Antiviral activity against HIV 1 3B harboring integrase E92Q, S230N and L34M triple mutant infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay selected after 60 passages in presence of compound
    [PMID: 18378713]
    MT4 EC50
    0.9 μM
    Compound: 49
    Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay
    Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of viral replication after 5 days by MTT assay
    [PMID: 19719237]
    MT4 CC50
    1.15 μM
    Compound: 2, elvitegravir, GS-9137
    Cytotoxicity against human MT4 cells by MTT assay
    Cytotoxicity against human MT4 cells by MTT assay
    [PMID: 18665580]
    MT4 IC50
    1.3 nM
    Compound: EVG
    Inhibition of wild type HIV1 3B infected in human MT4 cells using cells pre-incubated with compound for 1 hr measured 4 days post viral infection by MTT assay
    Inhibition of wild type HIV1 3B infected in human MT4 cells using cells pre-incubated with compound for 1 hr measured 4 days post viral infection by MTT assay
    [PMID: 22963135]
    MT4 CC50
    2.12 μM
    Compound: 1, GS-9137
    Cytotoxicity against human MT4 cells by MTT assay
    Cytotoxicity against human MT4 cells by MTT assay
    [PMID: 21227550]
    MT4 EC50
    2.12 μM
    Compound: 2, GS-9137
    Cytotoxicity against human MT4 cells by MTT assay
    Cytotoxicity against human MT4 cells by MTT assay
    [PMID: 20630765]
    MT4 CC50
    2.12 μM
    Compound: GS-9137
    Cytotoxicity against human MT4 cells by MTT assay
    Cytotoxicity against human MT4 cells by MTT assay
    [PMID: 18541726]
    MT4 IC50
    29 nM
    Compound: EVG
    Inhibition of wild type HIV1 3B infected in human MT4 cells using cells pre-incubated with compound for 1 hr measured 4 days post viral infection in presence of 20 mg/ml HSA by MTT assay
    Inhibition of wild type HIV1 3B infected in human MT4 cells using cells pre-incubated with compound for 1 hr measured 4 days post viral infection in presence of 20 mg/ml HSA by MTT assay
    [PMID: 22963135]
    MT4 CC50
    4 μM
    Compound: 49
    Cytotoxicity against human MT4 cells after 5 days by MTT assay
    Cytotoxicity against human MT4 cells after 5 days by MTT assay
    [PMID: 19719237]
    MT4 CC50
    4.6 μM
    Compound: 3, EVG
    Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay
    Cytotoxicity against mock-infected human MT4 cells after 5 days by MTT assay
    [PMID: 25907370]
    MT4 CC50
    6.3 μM
    Compound: EVG
    Cytotoxic activity against mock-infected human MT4 cellls assessed as reduction in cell viability by MTT assay
    Cytotoxic activity against mock-infected human MT4 cellls assessed as reduction in cell viability by MTT assay
    [PMID: 28951095]
    体外研究
    (In Vitro)

    Elvitegravir (GS-9137; JTK-303; D06677) 通过抑制 DNA 链转移来阻断 HIV-1 cDNA 的整合。 Elvitegravir 不仅对野生型毒株而且对耐药临床分离株都具有强大的抗 HIV 活性。 有趣的是,Elvitegravir 还显示出对鼠白血病病毒 (MLV) 和猿猴免疫缺陷病毒 (SIV) 的抗病毒活性。 Elvitegravir 对三种实验室 HIV 菌株显示出有效的抗病毒活性,EC50 值在亚纳摩尔到纳摩尔范围内。 接下来,针对代表各种 HIV-1 亚型的野生型临床分离株评估了 Elvitegravir 的活性。 Elvitegravir 抑制所有测试的 HIV-1 亚型的复制,抗病毒 EC50 范围为 0.1 至 1.26 nM。 此外,Elvitegravir 抑制携带 NRTI、NNRTI 和 PI 抗性相关基因型的 HIV-1 临床分离株的复制,对照 IN 抑制剂化合物 L-870,810 也是如此。 这些抑制剂的细胞毒性也使用 MTT 比色法测定。 在从三个独立供体获得的 PBMC 中,Elvitegravir 和 L-870,810 将靶细胞活力抑制 50% 的浓度平均值分别为 4.6±0.5 μM 和 2.7±0.6 μM。 因此,Elvitegravir 可以抑制多种 HIV 毒株,包括多种 HIV-1 亚型和携带与目前批准的抗逆转录病毒药物耐药性相关的多种突变的临床分离株[1]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    447.88

    Formula

    C23H23ClFNO5

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    埃替格韦

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 233.33 mg/mL (520.97 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.2327 mL 11.1637 mL 22.3274 mL
    5 mM 0.4465 mL 2.2327 mL 4.4655 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (5.58 mM); 悬浊液; 超声助溶

      此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.64 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.90%

    参考文献
    Cell Assay
    [1]

    MT-2 cells (2×105 cells) are infected with HIV-1 IIIB and then cultured in the presence of 0.5 nM or 0.1 nM Elvitegravir. Cultures are incubated at 37°C until an extensive cytopathic effect (CPE) is observed, and the culture supernatant is then harvested for further passage in fresh MT-2 cells. The concentration of Elvitegravir is increased when a significant CPE is observed. At the indicated passages, proviral DNA is extracted from infected MT-2 cells and then subjected to PCR, followed by direct population-based sequencing. Susceptibility to Elvitegravir at the indicated passages is determined using the MAGI assay or p24 production[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2327 mL 11.1637 mL 22.3274 mL 55.8185 mL
    5 mM 0.4465 mL 2.2327 mL 4.4655 mL 11.1637 mL
    10 mM 0.2233 mL 1.1164 mL 2.2327 mL 5.5819 mL
    15 mM 0.1488 mL 0.7442 mL 1.4885 mL 3.7212 mL
    20 mM 0.1116 mL 0.5582 mL 1.1164 mL 2.7909 mL
    25 mM 0.0893 mL 0.4465 mL 0.8931 mL 2.2327 mL
    30 mM 0.0744 mL 0.3721 mL 0.7442 mL 1.8606 mL
    40 mM 0.0558 mL 0.2791 mL 0.5582 mL 1.3955 mL
    50 mM 0.0447 mL 0.2233 mL 0.4465 mL 1.1164 mL
    60 mM 0.0372 mL 0.1861 mL 0.3721 mL 0.9303 mL
    80 mM 0.0279 mL 0.1395 mL 0.2791 mL 0.6977 mL
    100 mM 0.0223 mL 0.1116 mL 0.2233 mL 0.5582 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
    Elvitegravir
    目录号:
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