Sitagliptin phosphate (Synonyms: 磷酸西他列汀; MK-0431 phosphate)

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Sitagliptin phosphate (MK-0431 phosphate) 是一种有效的 DPP4 抑制剂，在 Caco-2 细胞中，IC₅₀ 值为 19 nM。

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Sitagliptin phosphate Chemical Structure

CAS No. : 654671-78-0

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥476	In-stock
25 mg	￥433	In-stock
50 mg	￥623	In-stock
100 mg	￥880	In-stock
200 mg	￥1280	In-stock
500 mg	￥2088	In-stock
1 g		询价
5 g		询价

or 大包装询价

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Other Forms of Sitagliptin phosphate:

Sitagliptin-d₄ phosphate In-stock
Sitagliptin In-stock
Sitagliptin phosphate monohydrate In-stock
(S)-Sitagliptin phosphate 询价
(Rac)-Sitagliptin 询价

MCE 顾客使用本产品发表的 21 篇科研文献

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DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of DPP4 with an IC₅₀ of 19 nM in Caco-2 cell extracts^[1].

IC₅₀ & Target

DPP-4

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	11 μM Compound: MK-0431	Inhibition of human DPP8 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins Inhibition of human DPP8 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins	[PMID: 22853995]
HEK293	IC₅₀	20 μM Compound: MK-0431	Inhibition of human DPP9 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins Inhibition of human DPP9 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins	[PMID: 22853995]
HEK293	IC₅₀	22 nM Compound: Sitagliptin Phosphate	Inhibition of recombinant human DPP-4 expressed in HEK293 cells using H-Gly-Pro-AMC as substrate measured over 15 mins by fluorescence analysis Inhibition of recombinant human DPP-4 expressed in HEK293 cells using H-Gly-Pro-AMC as substrate measured over 15 mins by fluorescence analysis	[PMID: 28128944]
HEK293	IC₅₀	6 nM Compound: MK-0431	Inhibition of human DPP4 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins Inhibition of human DPP4 expressed in HEK293 cells using Ala-Pro-p-nitroanilide hydrochloride salt as substrate preincubated for 10 mins prior to addition of substrate measured after 30 mins	[PMID: 22853995]

体外研究
(In Vitro)

Sitagliptin phosphate 对 Caco-2 细胞提取物中的 DPP-4 表现出有效的抑制作用，IC₅₀ 为 19 nM^[1]。西格列汀通过涉及 cAMP/PKA/Rac1 激活的通路减少分离的脾脏 CD4 T 细胞的体外迁移^[2]。最近的一项研究表明，西格列汀发挥一种新颖的直接作用，通过 DPP-4 独立的、蛋白激酶 A 和 MEK-ERK1/2 依赖的途径刺激肠道 L 细胞分泌 GLP-1。因此，它降低了自身免疫对移植物存活的影响^[3]。

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

体内研究
(In Vivo)

在自由喂养的 Han-Wistar 体内，Sitagliptin phosphate 抑制血浆 DPP-4 活性的 ED₅₀ 值计算为给药后 7 小时 2.3 mg/kg 和给药后 24 小时 30 mg/kg大鼠^[1]。
链脲佐菌素诱导的 1 型糖尿病小鼠模型显示血浆中 DPP-4 水平升高，这在服用 Sitagliptin phosphate 饮食的小鼠中可被显著抑制。这是通过对高血糖症的调节产生积极影响来实现的，可能是通过延长胰岛移植物的存活^[4]。
Sitagliptin phosphate 的血浆清除率和分布容积在大鼠中 (40-48 mL/min/kg，7-9 L/kg) 高于狗 (9 mL/min/kg，3 L/kg)；其半衰期在大鼠中较短，为 2 小时，而在狗中为 4 小时^[5]。

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

Clinical Trial

分子量

505.31

Formula

C₁₆H₁₈F₆N₅O₅P

CAS 号

654671-78-0

性状

固体

颜色

White to off-white

中文名称

磷酸西他列汀

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (197.90 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)

H₂O 中的溶解度 : 50 mg/mL (98.95 mM; 超声助溶)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9790 mL	9.8949 mL	19.7898 mL
5 mM	0.3958 mL	1.9790 mL	3.9580 mL
10 mM	0.1979 mL	0.9895 mL	1.9790 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.95 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.95 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 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。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.95 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 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玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。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： PBS
Solubility: 50 mg/mL (98.95 mM); 澄清溶液; 超声助溶

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

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

该产品水溶性佳，请具体参考实测水 / PBS / Saline 中的溶解度数据。

您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。

纯度 & 产品资料

纯度: 99.85%

选择批次：

Data Sheet (648 KB) SDS (393 KB)

COA (285 KB) LCMS (89 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Thomas, L., et al. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylm ethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of acti [Content Brief]

[2]. Kim, S.J., et al., Dipeptidyl peptidase IV inhibition with MK0431 improves islet graft survival in diabetic NOD mice partially via T-cell modulation. Diabetes, 2009. 58(3): p. 641-51. [Content Brief]

[3]. Sangle, G.V., et al., Novel biological action of the dipeptidylpeptidase-IV inhibitor, sitagliptin, as a glucagon-like peptide-1 secretagogue. Endocrinology, 2012. 153(2): p. 564-73. [Content Brief]

[4]. Kim, S.J., et al., Inhibition of dipeptidyl peptidase IV with sitagliptin (MK0431) prolongs islet graft survival in streptozotocin-induced diabetic mice. Diabetes, 2008. 57(5): p. 1331-9. [Content Brief]

[5]. Beconi, M.G., et al. Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs. Drug Metab Dispos, 2007. 35(4): p. 525-32. [Content Brief]

Cell Assay ^[2]	CD4T-cells are plated on membrane inserts in serum-free RPMI 1640, and cell migration is assayed using Transwell chambers (Corning), in the presence or absence of purified porcine kidney DPP-4 (32.1 units/mg; 100 mU/mL final concentration) and DPP-4 inhibitor (100 μM). After 1 hour, cells on the upper surface are removed mechanically, and cells that have migrated into the lower compartment are counted. The extent of migration is expressed relative to the control sample. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice: Overnight fasted C57BL/6J mice are challenged 45 min after compound administration with an oral glucose load (2 g/kg). Blood samples for glucose measurement are obtained by tail bleed predose and at serial time points after the glucose load. To evaluate the duration of the effect on glucose tolerance, vehicle or DPP-4 inhibitors are administered 16 h before the glucose challenge. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Thomas, L., et al. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylm ethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of acti [Content Brief] [2]. Kim, S.J., et al., Dipeptidyl peptidase IV inhibition with MK0431 improves islet graft survival in diabetic NOD mice partially via T-cell modulation. Diabetes, 2009. 58(3): p. 641-51. [Content Brief] [3]. Sangle, G.V., et al., Novel biological action of the dipeptidylpeptidase-IV inhibitor, sitagliptin, as a glucagon-like peptide-1 secretagogue. Endocrinology, 2012. 153(2): p. 564-73. [Content Brief] [4]. Kim, S.J., et al., Inhibition of dipeptidyl peptidase IV with sitagliptin (MK0431) prolongs islet graft survival in streptozotocin-induced diabetic mice. Diabetes, 2008. 57(5): p. 1331-9. [Content Brief] [5]. Beconi, M.G., et al. Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs. Drug Metab Dispos, 2007. 35(4): p. 525-32. [Content Brief]

Sitagliptin phosphate 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.9790 mL	9.8949 mL	19.7898 mL	49.4746 mL
	5 mM	0.3958 mL	1.9790 mL	3.9580 mL	9.8949 mL
	10 mM	0.1979 mL	0.9895 mL	1.9790 mL	4.9475 mL
	15 mM	0.1319 mL	0.6597 mL	1.3193 mL	3.2983 mL
	20 mM	0.0989 mL	0.4947 mL	0.9895 mL	2.4737 mL
	25 mM	0.0792 mL	0.3958 mL	0.7916 mL	1.9790 mL
	30 mM	0.0660 mL	0.3298 mL	0.6597 mL	1.6492 mL
	40 mM	0.0495 mL	0.2474 mL	0.4947 mL	1.2369 mL
	50 mM	0.0396 mL	0.1979 mL	0.3958 mL	0.9895 mL
	60 mM	0.0330 mL	0.1649 mL	0.3298 mL	0.8246 mL
	80 mM	0.0247 mL	0.1237 mL	0.2474 mL	0.6184 mL
DMSO	100 mM	0.0198 mL	0.0989 mL	0.1979 mL	0.4947 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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.

Keywords:

Sitagliptin654671-78-0MK-0431磷酸西他列汀MK0431MK 0431Dipeptidyl PeptidaseAutophagyDPPInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Sitagliptin phosphate (Synonyms: 磷酸西他列汀; MK-0431 phosphate)

Customer Review

Other Forms of Sitagliptin phosphate:

MCE 顾客使用本产品发表的 21 篇科研文献