Murepavadin TFA POL7080 TFA|西域试剂

Murepavadin TFA POL7080 TFA,99.82%

产品编号：Bellancom-P1674A| 分子式：C₇₃H₁₁₂N₂₂O₁₆.C₂HF₃O₂| 分子量：1667.83

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-P1674A	￥3500.00	杭州北京（现货）
Bellancom-P1674A	￥5500.00	杭州北京（现货）
Bellancom-P1674A	￥16500.00	杭州北京（现货）
Bellancom-P1674A	￥22500.00	杭州北京（现货）

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Murepavadin TFA POL7080 TFA

产品介绍

Murepavadin (POL7080) (TFA)，一种 14 个氨基酸的环肽，是一种高效的特异性抗生素。Murepavadin 对 P. aeruginosa 表现出有效的抗菌活性。MIC₅₀ 和 MIC₉₀ 值均为 0.12 mg/L。Murepavadin 还可以靶向脂多糖转运蛋白 D。Murepavadin 可用于细菌耐药性的研究。

生物活性

Murepavadin (POL7080) (TFA), a 14-amino-acid cyclic peptide, is a highly potent, specific antibiotic. Murepavadin exhibits a potent antimicrobial activity for P. aeruginosa with MIC₅₀ and MIC₉₀ values both of 0.12 mg/L. Murepavadin also can target the lipopolysaccharide transport portin D. Murepavadin can be used for the research of bacterial resistance.

体外研究

Murepavadin has activity against P. aeruginosa with MIC₅₀ and MIC₉₀ values both of 0.12 mg/L.
Murepavadin inhibits megalin-mediated uptake of gentamicin in vitro with an IC₅₀ value of 5.84 μM.

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

体内研究

Murepavadin (s.c.; 0-100mg/kg) is active in pre-clinical animal models including infections with XDR isolates.

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

Animal Model:	Murine models of P. aeruginosa infection
Dosage:	0-100 mg/kg
Administration:	Subcutaneous, q24h or q12h
Result:	Resulted in an increase in survival rate to 100% and showed significantly lower CFU levels both in the blood and in the peritoneal fluid at 2 and 10 mg/kg 1 h post-infection.

Animal Model:	Mouse, rat, rabbit, and monkey
Dosage:	0-5 mg/kg
Administration:	Intraperitoneal or subcutaneous, single
Result:	Followed a two-compartment model following intravenous administration and decline of plasma concentrations. Distributed into the aqueous phase of the body, and systemic plasma clearance (CL) values were similar to the species-specific glomerular filtration rates (GFRs) . Had high bioavailability (67.79%) after subcutaneous (s.c.) administration in rats but had low oral bioavailability (<0.01%). Had a linear relationship between ELF AUC and unbound plasma AUC in mouse. Did not readily cross the blood/brain barrier.

体内研究

Murepavadin (s.c.; 0-100mg/kg) is active in pre-clinical animal models including infections with XDR isolates.

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

Animal Model:	Murine models of P. aeruginosa infection
Dosage:	0-100 mg/kg
Administration:	Subcutaneous, q24h or q12h
Result:	Resulted in an increase in survival rate to 100% and showed significantly lower CFU levels both in the blood and in the peritoneal fluid at 2 and 10 mg/kg 1 h post-infection.

Animal Model:	Mouse, rat, rabbit, and monkey
Dosage:	0-5 mg/kg
Administration:	Intraperitoneal or subcutaneous, single
Result:	Followed a two-compartment model following intravenous administration and decline of plasma concentrations. Distributed into the aqueous phase of the body, and systemic plasma clearance (CL) values were similar to the species-specific glomerular filtration rates (GFRs) . Had high bioavailability (67.79%) after subcutaneous (s.c.) administration in rats but had low oral bioavailability (<0.01%). Had a linear relationship between ELF AUC and unbound plasma AUC in mouse. Did not readily cross the blood/brain barrier.

性状

Solid

溶解性数据

In Vitro:

H₂O : 50 mg/mL (29.98 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.5996 mL	2.9979 mL	5.9958 mL
5 mM	0.1199 mL	0.5996 mL	1.1992 mL
10 mM	0.0600 mL	0.2998 mL	0.5996 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 (sealed storage, away from moisture)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶