JPE-1375

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JPE-1375

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1254036-23-1

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品介绍

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。

生物活性

JPE-1375 is acomplement C5a receptor 1(C5aR1) antagonist. JPE-1375 effectively inhibits polymorphonuclear leukocyte mobilization (EC₅₀=6.9 μM) and reducesTNFlevels (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 EC₅₀values 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].

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:

1.19Pharmacokinetic Parameters of JPE-1375 in C57BL/6J wild-type mice^[1].

	IV (1 mg/kg)
T_1/2(h)	0.13
C_max(μg/mL)	7.18
AUC_0-t(μg/mLoh)	2.40
AUC_{0-inf, obs}(μg/mLoh)	2.41
AUC_{0-t/0-inf, obs}(μg/mLoh)	1.00
AUMC_{0-inf, obs}(μg/mLoh²)	0.13
MRT_{0-inf, obs}(h)	0.05
V_{z, obs}((μg)/(μg/mL))	2.38
CL, obs ((μg)/(μg/mL)/h)	12.47
V_{ss, obs}((μg)/(μg/mL))	0.66

分子量

955.08

性状

Solid

Formula

C₄₉H₆₃FN₁₀O₉

CAS 号

1254036-23-1

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

In Vitro:

DMSO : 100 mg/mL(104.70 mM;Need ultrasonic)

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
10 mM	0.1047 mL	0.5235 mL	1.0470 mL

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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。