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SAG hydrochloride

رقم الكتالوجGC37580

هيدروكلوريد SAG هو ناهض قوي لمستقبلات (Smo) (EC50 = 3 نانومتر ؛ Kd = 59 نانومتر)ينشط SAG hydrochloride مسار إشارات القنفذ ويقاوم تثبيط السيكلوبامين لـ Smo

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SAG hydrochloride التركيب الكيميائي

Cas No.: 2095432-58-7

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
125٫00
متوفر
1mg
56٫00
متوفر
5mg
108٫00
متوفر
10mg
171٫00
متوفر
25mg
315٫00
متوفر
50mg
441٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of SAG hydrochloride

SAG (hydrochloride) is a potent Smo receptor agonist, and activates the Hedgehog signaling pathway, with a Kd of 59 nM. Kd: 59 nM (Smo)[1].

SAG (hydrochloride) acts downstream of Ptch1 in the Hh pathway and counteracts cyclopamine inhibition of Smo. SAG induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50 of 3 nM and then inhibits expression at higher concentrations. In Smo-expressing Cos-1 cells, SAG yields an apparent dissociation constant (KD) of 59 nM for the SAG/Smo complex[1]. SAG and purmorphamine verride the inhibitory effect of robotnikinin since Smo functions downstream of Shh/Ptc1[2].

In CD-1 mice, SAG (1.0 mM) or NELL-1 (600 μg/ml) alone results in increased bone formation at 4 and 8 weeks, but significantly greater bone formation with both components combined (SAG + NELL-1). The combination of the two compounds exhibits a significant increase in new bone formation, accompanied by increased defect vascularization[3]. SAG (15, 17, or 20 mg/kg, i.p.) induces pre-axial polydactyly prevalently. The highest SAG dose is effective in ca. 80% of the embryos and increased Gli1 and Gli2 mRNA expression in the limb bud, with Gli1 mRNA being the most upregulated[4].

[1]. Chen JK, et al. Small molecule modulation of Smoothened activity. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6. [2]. Stanton BZ, et al. A small molecule that binds Hedgehog and blocks its signaling in human cells. Nat Chem Biol. 2009 Mar;5(3):154-6. [3]. Lee S, et al. Combining Smoothened Agonist (SAG) and NEL-like protein-1 (NELL-1) Enhances Bone Healing. Plast Reconstr Surg. 2017 Feb 13. [4]. Fish EW, et al. Preaxial polydactyly following early gestational exposure to the smoothened agonist, SAG, in C57BL/6J mice. Birth Defects Res A Clin Mol Teratol. 2016 Nov 1.

Chemical Properties of SAG hydrochloride

Cas No. 2095432-58-7 SDF
Canonical SMILES O=C(C1=C(Cl)C2=CC=CC=C2S1)N([C@H]3CC[C@H](NC)CC3)CC4=CC=CC(C5=CC=NC=C5)=C4.Cl
Formula C28H29Cl2N3OS M.Wt 526.52
الذوبان H2O : 25 mg/mL (47.48 mM; Need ultrasonic); DMSO : 21.67 mg/mL (41.16 mM; Need ultrasonic) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of SAG hydrochloride

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.8993 mL 9.4963 mL 18.9926 mL
5 mM 0.3799 mL 1.8993 mL 3.7985 mL
10 mM 0.1899 mL 0.9496 mL 1.8993 mL
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In vivo Formulation Calculator (Clear solution) of SAG hydrochloride

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Review for SAG hydrochloride

Average Rating: 5 ★★★★★ (Based on Reviews and 12 reference(s) in Google Scholar.)

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