1. Immunology/Inflammation
  2. Complement System
  3. JPE-1375

JPE-1375 是一种补体 C5a 受体 1 (C5aR1) 拮抗剂。JPE-1375 能有效抑制小鼠体内多形核白细胞动员 (EC50=6.9 µM) 和降低 TNF 水平 (EC50=4.5 µM)。JPE-1375 可用于自身免疫性和炎性疾病的研究。

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JPE-1375 Chemical Structure

JPE-1375 Chemical Structure

CAS No. : 1254036-23-1

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Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JPE-1375 is a complement C5a receptor 1 (C5aR1) antagonist. JPE-1375 effectively inhibits polymorphonuclear leukocyte mobilization (EC50=6.9 µM) and reduces TNF levels (EC50=4.5 µM) in mice. JPE-1375 can be used in studies of autoimmune and inflammatory diseases[1].

IC50 & Target

C5aR1[1].

体内研究
(In Vivo)

JPE-1375 (0.3, 1.0, 3.0 mg/kg; i.v.; single) inhibits PMN (polymorphonuclear leukocytes) mobilization and TNF with EC50 values of 6.9 and 4.5 µM, respectively[1].
JPE-1375 (1 mg/kg; i.v.; single) demonstrates a rapid distribution in the plasma, followed by elimination in mice[1].
JPE-1375 (1 mg/kg; i.v.; single) shows a strong negative correlation between PMN mobilization and TNF production with plasma concentrations[1].

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

Animal Model: C57BL/6J wild-type (10 to 12-week-old; C5a pharmacodynamic model)[1].
Dosage: 0.3, 1.0, 3.0 mg/kg
Administration: Intravenous injection; single.
Result: Significantly decreased C5a-mediated PMN mobilization at 1 and 3 mg/kg doses, while no effect was observed at a 0.3 mg/kg dose.
Showed a significant reduction in TNF plasma levels at 1 and 3 mg/kg dose with both compounds reducing C5a-mediated TNF by about 90%.
Animal Model: C57BL/6J wild-type mice(10 to 12-week-old)[1].
Dosage: 1 mg/kg
Administration: Intravenous injection; single.
Result: 1.19 Pharmacokinetic Parameters of JPE-1375 in C57BL/6J wild-type mice[1].
IV (1 mg/kg)
T1/2 (h) 0.13
Cmax (µg/mL) 7.18
AUC0-t (μg/mL•h) 2.40
AUC0-inf, obs (μg/mL•h) 2.41
AUC0-t/0-inf, obs (μg/mL•h) 1.00
AUMC0-inf, obs (μg/mL•h2) 0.13
MRT0-inf, obs (h) 0.05
Vz, obs ((μg)/(μg/mL)) 2.38
CL, obs ((μg)/(μg/mL)/h) 12.47
Vss, obs ((μg)/(μg/mL)) 0.66
分子量

955.08

Formula

C49H63FN10O9

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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (104.70 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 1.0470 mL 5.2352 mL 10.4703 mL
5 mM 0.2094 mL 1.0470 mL 2.0941 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 (protect from 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。

  • 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

纯度: 99.94%

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, 6 months; -20°C, 1 month (protect from 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.0470 mL 5.2352 mL 10.4703 mL 26.1758 mL
5 mM 0.2094 mL 1.0470 mL 2.0941 mL 5.2352 mL
10 mM 0.1047 mL 0.5235 mL 1.0470 mL 2.6176 mL
15 mM 0.0698 mL 0.3490 mL 0.6980 mL 1.7451 mL
20 mM 0.0524 mL 0.2618 mL 0.5235 mL 1.3088 mL
25 mM 0.0419 mL 0.2094 mL 0.4188 mL 1.0470 mL
30 mM 0.0349 mL 0.1745 mL 0.3490 mL 0.8725 mL
40 mM 0.0262 mL 0.1309 mL 0.2618 mL 0.6544 mL
50 mM 0.0209 mL 0.1047 mL 0.2094 mL 0.5235 mL
60 mM 0.0175 mL 0.0873 mL 0.1745 mL 0.4363 mL
80 mM 0.0131 mL 0.0654 mL 0.1309 mL 0.3272 mL
100 mM 0.0105 mL 0.0524 mL 0.1047 mL 0.2618 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:
JPE-1375
目录号:
HY-148141
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