2. GPCR/G Protein
  3. P2Y Receptor
  4. PPTN

PPTN 是一种有效，高亲和力，竞争性和高选择性的 P2Y14 受体拮抗剂，KB 为 434 pM。PPTN 对 P2Y1，P2Y2，P2Y4，P2Y6，P2Y11，P2Y12 或 P2Y13 受体无激动剂或拮抗剂作用。具有抗炎和免疫活性。

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PPTN Chemical Structure

PPTN Chemical Structure

CAS No. : 1160271-30-6

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规格 价格 是否有货 数量
5 mg ￥1183
In-stock
10 mg ￥2000
In-stock
25 mg ￥3900
In-stock
1 mg 询价

* Please select Quantity before adding items.

Customer Review

Other Forms of PPTN:

PPTN 相关抗体

Top Publications Citing Use of Products

    PPTN purchased from MCE. Usage Cited in: Int Immunopharmacol. 2022 Nov 30;114:109507.  [Abstract]

    HQL6 or PPTN significantly decreases the expressions of NLRP3, ASC and caspase-1 p20 in synovial tissue of rats.

    PPTN purchased from MCE. Usage Cited in: Int Immunopharmacol. 2022 Nov 30;114:109507.  [Abstract]

    HQL6 or PPTN significantly decreases the colocalization of NLRP3 and ASC in synovial tissues of rats. NLRP3 protein, ASC protein and nucleus are marked with Alexa Fluor 488 (Green), Alexa Fluor 647 (Red) and DAPI (Blue), respectively.

    查看 P2Y Receptor 亚型特异性产品:

    查看所有亚型
    P2Y1 Receptor P2Y2 Receptor P2Y6 Receptor P2Y12 Receptor P2Y13 Receptor P2Y14 Receptor

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    PPTN is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. PPTN exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and immune activity[1].

    IC50 & Target

    KB: 434 pM (P2Y14 receptor)[1]
    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    CHO IC50
    14.5 nM
    Compound: 1
    Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6.5 by flow cytomtery based competitive fluorescence assay
    Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6.5 by flow cytomtery based competitive fluorescence assay
    		[PMID: 32787142]
    CHO IC50
    19 nM
    Compound: 1
    Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6 by flow cytomtery based competitive fluorescence assay
    Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 6 by flow cytomtery based competitive fluorescence assay
    		[PMID: 32787142]
    CHO IC50
    6 nM
    Compound: 3; PPTN
    Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R express
    Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R express
    		[PMID: 27331270]
    CHO IC50
    6 nM
    Compound: 1
    Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed
    Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from human P2Y14 expressed
    		[PMID: 32551012]
    CHO IC50
    9.75 nM
    Compound: 1
    Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7 by flow cytomtery based competitive fluorescence assay
    Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7 by flow cytomtery based competitive fluorescence assay
    		[PMID: 32787142]
    HEK293 IC50
    21.6 nM
    Compound: 1
    Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14
    Displacement of Alexafluor488 labeled 4-(4-(1-(4-(1-(6-(4-(6-amino-3-imino-4,5-disulfo-3H-xanthen-9-yl)-3-carboxybenzamido)hexyl)-1H-1,2,3-triazol-4-yl)butyl)piperidin-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoic acid from HA-tagged mouse P2Y14
    		[PMID: 32551012]
    HEK293 IC50
    21.6 nM
    Compound: 1
    Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
    Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
    		[PMID: 32787142]
    体外研究
    (In Vitro)

    PPTN exhibits strong selectivity for the P2Y14-R over the other seven nucleotide-activated P2Y receptors. 1 μM PPTN exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors[1].
    PPTN inhibits UDP-glucose-promoted chemotaxis in differentiated HL-60 human promyelocytic leukemia cells with IC50s of ~1 nM in the presence of 10 μM UDP-glucose and ~4 nM in the presence of 100 μM[1].
    PPTN (10 µM) significantly decreases the ratios of p-ERK1/2 to ERK1/2 and p-p38 to p38[2].

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

    PPTN 相关抗体:
    分子量

    475.50

    Formula

    C29H24F3NO2
    CAS 号
    性状

    固体

    颜色

    White to off-white

    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 6 months
    -20°C 1 month
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 22.22 mg/mL (46.73 mM; adjust pH to 7 with 1 M HCL; 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 2.1030 mL 10.5152 mL 21.0305 mL
    5 mM 0.4206 mL 2.1030 mL 4.2061 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。-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。

    • 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

    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
    纯度 & 产品资料
    参考文献

    PPTN 相关分类

    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。-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。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1030 mL 10.5152 mL 21.0305 mL 52.5762 mL
    5 mM 0.4206 mL 2.1030 mL 4.2061 mL 10.5152 mL
    10 mM 0.2103 mL 1.0515 mL 2.1030 mL 5.2576 mL
    15 mM 0.1402 mL 0.7010 mL 1.4020 mL 3.5051 mL
    20 mM 0.1052 mL 0.5258 mL 1.0515 mL 2.6288 mL
    25 mM 0.0841 mL 0.4206 mL 0.8412 mL 2.1030 mL
    30 mM 0.0701 mL 0.3505 mL 0.7010 mL 1.7525 mL
    40 mM 0.0526 mL 0.2629 mL 0.5258 mL 1.3144 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.

    Keywords:

    PPTN1160271-30-6P2Y ReceptorP2Y14Anti-inflammatoryimmunep-ERK1/2ERK1/2p-p38p38Inhibitorinhibitorinhibit

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    目录号：
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