JPE-1375|cas:1254036-23-1|西域试剂

JPE-1375,99.94%

产品编号：Bellancom-148141| CAS NO：1254036-23-1| 分子式：C₄₉H₆₃FN₁₀O₉| 分子量：955.08

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-148141	￥1500.00	杭州北京（现货）
Bellancom-148141	￥2500.00	杭州北京（现货）
Bellancom-148141	￥5500.00	杭州北京（现货）
Bellancom-148141	￥8500.00	杭州北京（现货）
Bellancom-148141	￥13500.00	杭州北京（现货）

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JPE-1375

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 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.

体外研究

体内研究

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.
JPE-1375 (1 mg/kg; i.v.; single) demonstrates a rapid distribution in the plasma, followed by elimination in mice.
JPE-1375 (1 mg/kg; i.v.; single) shows a strong negative correlation between PMN mobilization and TNF production with plasma concentrations.

西域 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).
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).

Dosage:

1 mg/kg

Administration:

Intravenous injection; single.

Result:

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

	IV (1 mg/kg)
T_1/2 (h)	0.13
C_max (µg/mL)	7.18
AUC_0-t (μg/mL•h)	2.40
AUC_{0-inf, obs} (μg/mL•h)	2.41
AUC_{0-t/0-inf, obs} (μg/mL•h)	1.00
AUMC_{0-inf, obs} (μg/mL•h²)	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

体内研究

西域 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).
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).

Dosage:

1 mg/kg

Administration:

Intravenous injection; single.

Result:

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

	IV (1 mg/kg)
T_1/2 (h)	0.13
C_max (µg/mL)	7.18
AUC_0-t (μg/mL•h)	2.40
AUC_{0-inf, obs} (μg/mL•h)	2.41
AUC_{0-t/0-inf, obs} (μg/mL•h)	1.00
AUMC_{0-inf, obs} (μg/mL•h²)	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

性状

Solid

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°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。

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)

参考文献