GlpBio

SAG

目录号: GC12068纯度: >99.50%同义词: Smoothened Agonist
SAG(Smoothened Agonist)是一种有效的Smo受体激动剂。
SAG
Cas No.: 912545-86-9
规格价格库存数量操作
1mg¥420.00现货
1
5mg¥1,260.00现货
1
10mg¥2,030.00现货
1
25mg¥2,450.00现货
1
50mg¥3,430.00现货
1
10mM (in 1mL DMSO)¥1,359.00现货
1
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产品描述 Description

SAG (Smoothened Agonist) is an effective Smo receptor agonist. SAG activates the Hedgehog signaling pathway. SAG induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50 of 3nM. In Cos-1 cells expressing Smo, SAG has a Kd of 59nM for the SAG/Smo complex[1-3].

SAG (250nM; 24h) promotes migration of MDA-MB-231 cells[4]. SAG(1μM; 6 days) treatment rescues mitochondrial dysfunction in FXN-deficient astrocytes[5].

SAG(15-20mg/kg；ip) generally induces preaxial polydactylism in a dose-dependent manner in mice[6]. SAG(20μg/g body weight; i.p; 3 times) restores Shh(Sonic hedgehog) signaling, leading to the rescue of BBB function in HIV-infected, humanized mice[7].

References:
[1]. Chen JK, Taipale J, et,al. Small molecule modulation of Smoothened activity. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6. doi: 10.1073/pnas.182542899. Epub 2002 Oct 21. PMID: 12391318; PMCID: PMC137838.
[2]. Bragina O, Sergejeva S, et,al. Smoothened agonist augments proliferation and survival of neural cells. Neurosci Lett. 2010 Sep 27;482(2):81-5. doi: 10.1016/j.neulet.2010.06.068. Epub 2010 Jul 1. PMID: 20600593.
[3]. Stanton BZ, Peng LF, et,al. A small molecule that binds Hedgehog and blocks its signaling in human cells. Nat Chem Biol. 2009 Mar;5(3):154-6. doi: 10.1038/nchembio.142. Epub 2009 Jan 18. PMID: 19151731; PMCID: PMC2770933.
[4]. Guerrini G, Criscuoli M, et,al. Inhibition of smoothened in breast cancer cells reduces CAXII expression and cell migration. J Cell Physiol. 2018 Dec;233(12):9799-9811. doi: 10.1002/jcp.26947. Epub 2018 Aug 21. PMID: 30132883.
[5]. Vicente-Acosta A, Giménez-Cassina A, et,al. The smoothened agonist SAG reduces mitochondrial dysfunction and neurotoxicity of frataxin-deficient astrocytes. J Neuroinflammation. 2022 Apr 12;19(1):93. doi: 10.1186/s12974-022-02442-w. PMID: 35413853; PMCID: PMC9006607.
[6]. Fish EW, Parnell SE et,al. Preaxial polydactyly following early gestational exposure to the smoothened agonist, SAG, in C57BL/6J mice. Birth Defects Res. 2017 Jan 20;109(1):49-54. doi: 10.1002/bdra.23571. PMID: 27801979; PMCID: PMC5388559.
[7]. Singh VB, Singh MV, et,al. Smoothened Agonist Reduces Human Immunodeficiency Virus Type-1-Induced Blood-Brain Barrier Breakdown in Humanized Mice. Sci Rep. 2016 May 31;6:26876. doi: 10.1038/srep26876. PMID: 27241024; PMCID: PMC4886511.

SAG(Smoothened Agonist)是一种有效的Smo受体激动剂。SAG能够激活 Hedgehog 信号通路。SAG在Shh-LIGHT2细胞中可促使萤火虫荧光素酶的表达，EC50为3nM。在表达Smo的Cos-1细胞中，SAG与SAG/Smo复合物的Kd为59nM[1-3]。

SAG(250nM;24h)促进MDA-MB-231细胞的迁移[4]。SAG(1μM; 6 days)治疗可挽救FXN缺陷的星形胶质细胞线粒体功能障碍[5]。

SAG(15-20mg/kg；ip) 在小鼠中以剂量依赖性方式普遍诱导轴前多指畸形[6]。在HIV感染的人源化小鼠中，SAG(20μg/g body weight; i.p; 3 times)恢复Shh(Sonic hedgehog)信号，导致血脑屏障功能的恢复[7]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

MDAMB 231 cells

Preparation Method

Cells were seeded at a concentration of 2 × 105 cells in 12 well/plates. When treated with compounds, cells were pretreated for 24h with SAG 250nM or DMSO as a control. The day after, a scratch was done using a p200 tip to the confluent monolayer; cells were then washed with PBS and resuspended in 1ml RPMI supplemented with 10% FBS and AraC (Cytosine β-D-arabinofuranoside; a selective inhibitor of DNA synthesis; 2.5µg/ml).

Reaction Conditions

250nM;24h

Applications

SAG promotes migration of MDA-MB-231 cells.

Animal experiment [2]:

Animal models

HIV-infected, humanized mice

Preparation Method

Mice were injected on alternate days with SAG (20μg/g body weight) or vehicle control, DMSO, for a total of 3 injections. Evans blue exclusion assay was performed to measure BBB permeability.

Dosage form

20μg/g body weight; i.p; 3 times

Applications

SAG rescues BBB(Blood Brain Barrier) integrity.

References:
[1]. Guerrini G, Criscuoli M, et,al. Inhibition of smoothened in breast cancer cells reduces CAXII expression and cell migration. J Cell Physiol. 2018 Dec;233(12):9799-9811. doi: 10.1002/jcp.26947. Epub 2018 Aug 21. PMID: 30132883.
[2]. Singh VB, Singh MV, et,al. Smoothened Agonist Reduces Human Immunodeficiency Virus Type-1-Induced Blood-Brain Barrier Breakdown in Humanized Mice. Sci Rep. 2016 May 31;6:26876. doi: 10.1038/srep26876. PMID: 27241024; PMCID: PMC4886511.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
912545-86-9
同义词
Smoothened Agonist
化学名
3-chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide
SMILES
CN[C@@]1([H])CC[C@@](N(C(C2=C(Cl)C3=CC=CC=C3S2)=O)CC4=CC(C5=CC=NC=C5)=CC=C4)([H])CC1
分子式
C28H28ClN3OS
分子量
490.06 g/mol
溶解性
≥ 24.5mg/mL in DMSO, ≥ 16.3mg/mL in Water with ultrasonic and warming
保存条件
4°C, protect from light
General tips
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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol