1. GPCR/G Protein
  2. Succinate Receptor 1
  3. hGPR91 antagonist 1

hGPR91 antagonist 1 

目录号: HY-126217 纯度: 98.71%
COA 产品使用指南

hGPR91 Antagonist 1 (Compound 4c) 是一种有效的 GPR91 拮抗剂,对于人 GPR91 的 IC50 为 7 nM。

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hGPR91 antagonist 1 Chemical Structure

hGPR91 antagonist 1 Chemical Structure

CAS No. : 1314796-00-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2446
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1 mg ¥860
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5 mg ¥2100
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10 mg ¥3100
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25 mg ¥5200
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

hGPR91 antagonist 1 (Compound 4c) is a potent and selective GPR91 antagonist with an IC50 of 7 nM for human GPR91[1].

IC50 & Target

IC50: 7 μM (HGPR91)[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO-K1 IC50
> 30 μM
Compound: 4c
Antagonist activity at human GPR99 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level at by FLIPR assay
Antagonist activity at human GPR99 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level at by FLIPR assay
[PMID: 21571530]
CHO-K1 IC50
7 nM
Compound: 4c
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
Antagonist activity at human GPR91 receptor expressed in CHO-K1 cells co-expressing Galpha and Gqi5 G-protein assessed as inhibition of succinate-induced increase in intracellular calcium level by FLIPR assay
[PMID: 21571530]
体内研究
(In Vivo)

HGPR91 antagonist 1 (Compound 4c) 在 2、4 小时分别导致 ΔMAP 抑制率为 59%、76%,并显示大鼠血浆蛋白结合率为 99%。 HGPR91 antagonist 1 在体内条件下与靶标结合,RLM 清除率 (CL) 为 0.2 nmol/min/mg[1]

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

Animal Model: Wistar rats[1]
Dosage: 100 mg/kg
Administration: I.p.; 2 and 4 hours
Result: Led to 59 and 76% inhibition of ΔMAP at 2 and 4 hours.
分子量

529.53

Formula

C31H23F4N3O

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 : ≥ 125 mg/mL (236.06 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8885 mL 9.4423 mL 18.8847 mL
5 mM 0.3777 mL 1.8885 mL 3.7769 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

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

hGPR91 antagonist 1 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 1.8885 mL 9.4423 mL 18.8847 mL 47.2117 mL
5 mM 0.3777 mL 1.8885 mL 3.7769 mL 9.4423 mL
10 mM 0.1888 mL 0.9442 mL 1.8885 mL 4.7212 mL
15 mM 0.1259 mL 0.6295 mL 1.2590 mL 3.1474 mL
20 mM 0.0944 mL 0.4721 mL 0.9442 mL 2.3606 mL
25 mM 0.0755 mL 0.3777 mL 0.7554 mL 1.8885 mL
30 mM 0.0629 mL 0.3147 mL 0.6295 mL 1.5737 mL
40 mM 0.0472 mL 0.2361 mL 0.4721 mL 1.1803 mL
50 mM 0.0378 mL 0.1888 mL 0.3777 mL 0.9442 mL
60 mM 0.0315 mL 0.1574 mL 0.3147 mL 0.7869 mL
80 mM 0.0236 mL 0.1180 mL 0.2361 mL 0.5901 mL
100 mM 0.0189 mL 0.0944 mL 0.1888 mL 0.4721 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:
hGPR91 antagonist 1
目录号:
HY-126217
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