Smoothened Agonist (SAG)

Alias:

SAG free base;SAG; SAG (cyclopamine antagonist); SAG (Smo agonist)

Cat No.:V1338 Purity: ≥98%
Smoothened Agonist (SAG), a benzothiophene analog, is a potent and cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.
Smoothened Agonist (SAG) Chemical Structure CAS No.: 912545-86-9
Product category: Hedgehog(Smoothened) ROCK
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
2mg
5mg
10mg
25mg
50mg
100mg
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Other Forms of Smoothened Agonist (SAG):

  • SAG hydrochloride
  • SAG dihydrochloride
  • (Rac)-SAG
Official Supplier of:
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Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Purity: ≥98%

Product Description

Smoothened Agonist (SAG), a benzothiophene analog, is a potent and cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells. In Shh-light 2 cells, SAG significantly (EC50 ~ 3 nM) activates the Hedgehog signaling pathway. Ptch proteins are not necessary for SAG to cause pathway activation. The hedgehog pathway, which is connected to both normal development and carcinogenesis, uses the Smoothened receptor (SMO) to mediate signal transduction. Certain tumors' growth can be inhibited by SMO antagonists.

Biological Activity I Assay Protocols (From Reference)
Targets
Smo ( EC50 = 3 nM )
ln Vitro

In vitro activity: SAG can mitigate the antagonistic effects of glucocorticoids (GCs) on the proliferation of granule neuron precursors (CGNPs), which is driven by Shh.[2]

ln Vivo
Smoothened Agonist (SAG) administered systemically inhibits the neurotoxic effects of glucocorticoids. In vivo, Smoothened Agonist can activate Shh transcriptional targets by bridging the blood-brain barrier. Neonatal cerebellar developmental abnormalities induced by GC are effectively prevented by SAG at the treatment dose.[2]
Cell Assay
CGNP are stimulated by various SAG concentrations (15 to 240 nM) compared with ShhN (3 μg/ml) and vehicle after 24 hours in vitro. With the LightCycler 480, quantitative reverse transcription-PCR is carried out using SYBR Green master mix.
Animal Protocol
Rats: 2.5 nM, intracerebroventricular administration; Mice: 20 μg/g, i.p.
Rats and mice
References

[1]. Proc Natl Acad Sci U S A . 2002 Oct 29;99(22):14071-6.

[2]. Sci Transl Med . 2011 Oct 19;3(105):105ra104.

[3]. Birth Defects Res . 2017 Jan 20;109(1):49-54.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C28H28CLN3OS
Molecular Weight
490.06
Exact Mass
489.16
Elemental Analysis
C, 68.63; H, 5.76; Cl, 7.23; N, 8.57; O, 3.26; S, 6.54
CAS #
912545-86-9
Appearance
Powder
SMILES
CNC1CCC(CC1)N(CC2=CC(=CC=C2)C3=CC=NC=C3)C(=O)C4=C(C5=CC=CC=C5S4)Cl
InChi Key
VFSUUTYAEQOIMW-UHFFFAOYSA-N
InChi Code
InChI=1S/C28H28ClN3OS/c1-30-22-9-11-23(12-10-22)32(28(33)27-26(29)24-7-2-3-8-25(24)34-27)18-19-5-4-6-21(17-19)20-13-15-31-16-14-20/h2-8,13-17,22-23,30H,9-12,18H2,1H3
Chemical Name
3-chloro-N-[4-(methylamino)cyclohexyl]-N-[(3-pyridin-4-ylphenyl)methyl]-1-benzothiophene-2-carboxamide
Synonyms

SAG free base;SAG; SAG (cyclopamine antagonist); SAG (Smo agonist)

HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 71~98 mg/mL (134.8~200 mM)
Water: N/A
Ethanol: ~40 mg/mL (~75.9 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0406 mL 10.2028 mL 20.4057 mL
5 mM 0.4081 mL 2.0406 mL 4.0811 mL
10 mM 0.2041 mL 1.0203 mL 2.0406 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05823207 Not yet recruiting Other: sage essential oil Premenstrual Syndrome
Anxiety
Cansu Mine Aydin May 2023 Not Applicable
NCT04735419 Recruiting Other: No intervention Streptococcus Agalactiae Infection St George's, University of London December 1, 2021 N/A
NCT01888471 NCT01888471 Procedure: Blood sample
Other: Vaginal swab sample
Streptococcus Agalactiae GlaxoSmithKline December 11, 2013 Not Applicable
Biological Data
  • Alcian blue cartilage staining in representative forelimbs of embryos treated with SAG on GD 9.25. Birth Defects Res . 2017 Jan 20;109(1):49-54.
  • Figure 2A and 2B SAG dose-response for observable defects in GD15 embryos. Birth Defects Res . 2017 Jan 20;109(1):49-54.
  • Results of toxicity studies with SAG at treatment and high doses. Sci Transl Med . 2011 Oct 19;3(105):105ra104.
  • SAG treatment has no detrimental effect on lung maturation. Sci Transl Med . 2011 Oct 19;3(105):105ra104.
  • SAG acts downstream of Ptch1 in the Hh pathway and counteracts cyclopamine inhibition of Smo. Proc Natl Acad Sci U S A . 2002 Oct 29;99(22):14071-6.
  • SAG binds directly to Smo heptahelical bundle. Proc Natl Acad Sci U S A . 2002 Oct 29;99(22):14071-6.
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