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Chemical Structure| 2095432-58-7 Chemical Structure| 2095432-58-7

Structure of SAG HCl
CAS No.: 2095432-58-7

Chemical Structure| 2095432-58-7

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SAG hydrochloride is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM) that activates the Hedgehog signaling pathway and counteracts Cyclopamine inhibition of Smo.

Synonyms: SAG hydrochloride

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Product Details of SAG HCl

CAS No. :2095432-58-7
Formula : C28H29Cl2N3OS
M.W : 526.52
SMILES Code : 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.[H]Cl
Synonyms :
SAG hydrochloride
MDL No. :N/A
InChI Key :CRWTYWYPPITOOZ-UHFFFAOYSA-N
Pubchem ID :121540649

Safety of SAG HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of SAG HCl

Hedgehog

Isoform Comparison

Biological Activity

Description
SAG hydrochloride is a highly effective agonist of the Smoothened (Smo) receptor (EC50=3 nM; KD=59 nM). It activates the Hedgehog signaling pathway and antagonizes the inhibitory effects of Cyclopamine on Smo[1][2][3].

In Vitro:

Cell Line
Concentration Treated Time Description References
Primary hepatic cells 0.25–2.00 mM 1 h SAG pre-treatment significantly protected against cytotoxicity induced by CCl4 and significantly reduced AST and ALT levels. Int J Mol Sci. 2022 Apr 17;23(8):4429.
human adipose-derived mesenchymal stem cells (ASCs) 200 nM 24 h Activate the Hedgehog signaling pathway and detect the accumulation of Smo in cilia. Results showed that SAG treatment increased the accumulation of Smo in cilia, indicating the activation of the Hedgehog pathway. Stem Cell Reports. 2018 Feb 13;10(2):583-599.
NIH 3T3 cells 1 μM 48 h To detect defects in downstream Shh signaling in Chmp1a null and control MEFs, measured by Gli1 activation, showing no significant defect. Cell Rep. 2018 Jul 24;24(4):973-986.e8.
SVG-A cells 1 μM 48 h Activation of SHH signaling, inducing GLI1 and PTCH expression, showing no significant difference between CHMP1A null and WT cells. Cell Rep. 2018 Jul 24;24(4):973-986.e8.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Ick-mutant mice Intraperitoneal injection 20 mg/kg Single injection, embryos harvested between E12.5 and E18.5 By activating the SHH signaling pathway, SAG treatment successfully rescued congenital defects in Ick-mutant mice, including cleft palate. EBioMedicine. 2019 Nov;49:305-317
BALB/c mice Listeria infection model Subcutaneous injection 50 µg,100 μL Booster immunization 3 weeks after the first immunization To evaluate the immunological response and protective efficacy of archaeosome-encapsulated SAgs in BALB/c mice, the results showed that archaeosome-encapsulated SAgs significantly upregulated Th1 cytokine production and reduced bacterial burden in infected mice. Int J Nanomedicine. 2012;7:2433-47
Mice Cfp1d/d mouse model Intrauterine injection 1000 nM,10 μL Single injection, sacrificed at 3 or 21 hours SAG successfully rescued aberrant uterine cell proliferation and gene expression in Cfp1d/d female mice. Nat Commun. 2023 Jun 3;14(1):3220
Mice MCAo model Gavage 10mg/kg Once daily for 6 days To evaluate the role of SAG in post-stroke functional recovery, results showed that SAG treatment significantly improved motor and cognitive functions and increased the survival of newly generated cells. Stroke. 2017 Jun;48(6):1636-1645
Mice CCl4-induced liver injury model Oral 30 mg/kg Twice a week for 8 weeks SAG significantly restored SOD activity, GSH levels, and GPx activity, while it strongly reduced GSSG levels, lipid peroxidation, and H2O2 and ROS levels. SAG also reduced inflammation and fibrosis, improved liver function and mitophagy. Int J Mol Sci. 2022 Apr 17;23(8):4429.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.90mL

0.38mL

0.19mL

9.50mL

1.90mL

0.95mL

18.99mL

3.80mL

1.90mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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