BIP-135

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BIP-135

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:

941575-71-9

BIP-135 是一个高效、选择性的，ATP 竞争性的GSK-3抑制剂，对 GSK-3α 和 GSK-3β 作用的IC₅₀值分别为 16 nM 和 21 nM。BIP 135 具有神经保护作用。

生物活性

BIP-135 is a potent and selective ATP-competitiveGSK-3inhibitor, withIC₅₀s of 16 nM and 21 nM forGSK-3αandGSK-3β, respectively. BIP 135 exhibits neuroprotective effect^[1].

IC₅₀& Target

GSK-3α

16 nM (IC₅₀)

GSK-3β

21 nM (IC₅₀)

体外研究
(In Vitro)

BIP-135 (20-30 μM; 72 hours) increases the survival motor neuron (SMN) protein levels at a dose of 25 μM in human SMA fibroblasts. And the typical bell-shaped dose-response curve is observed due to some toxicity at higher concentrations^[1].
BIP-135 (20 μM; 48 hours) is a superior neuroprotective agent in the model of oxidative stress^[1].

Western Blot Analysis^[1]

Cell Line:	Human SMA fibroblasts
Concentration:	20 μM, 25 μM, 30 μM
Incubation Time:	72 hours
Result:	Led to a 7-fold increase in SMN levels at 25 μM.

体内研究
(In Vivo)

BIP-135 does not appear to be toxic and was well-tolerated by the animals (no decrease in body weight)^[1].
BIP-135 (75 mg/kg; i.p.; daily; from postnatal day 0 to 21) prolongs the median survival time of Δ7 SMA KO mouse model of spinal muscular atrophy^[1].

Animal Model:	Male and female SMN2^+/+, SMN2Δ7^+/+, Smn^+/–mice^[1]
Dosage:	75 mg/kg
Administration:	Intraperitoneal injection; daily; from postnatal day 0 to 21
Result:	Caused a modest extension in the median survival of SMA KO animals by two days.

分子量

421.24

性状

Solid

Formula

C₂₁H₁₃BrN₂O₃

CAS 号

941575-71-9

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

In Vitro:

DMSO : 62.5 mg/mL(148.37 mM;ultrasonic and warming and heat to 70℃)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.3739 mL	11.8697 mL	23.7394 mL
5 mM	0.4748 mL	2.3739 mL	4.7479 mL
10 mM	0.2374 mL	1.1870 mL	2.3739 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。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。