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SAG dihydrochloride

Cat No.:V69129 Purity: ≥98%
SAG di-HCl is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM).
SAG dihydrochloride
SAG dihydrochloride Chemical Structure CAS No.: 2702366-44-5
Product category: Smo
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
50mg
Other Sizes

Other Forms of SAG dihydrochloride:

  • Smoothened Agonist (SAG)
  • SAG hydrochloride
  • (Rac)-SAG
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
SAG di-HCl is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG di-HCl activates the Hedgehog signaling pathway and counteracts the inhibitory effect of Cyclopamine on Smo.
Biological Activity I Assay Protocols (From Reference)
Targets
EC50: 3 nM (Smo)[1]
ln Vitro
With an EC50 of 3 nM, SAG (0.1 nM-100 μM; 30 h) stimulates firefly luciferase expression in Shh-LIGHT2 cells, which is subsequently inhibited at higher concentrations[1]. When SAG (1-1000 nM; 1 h) competes with BODIPY-cyclopamine to bind to Smo-expressing Cos-1 cells, the SAG/Smo complex has an apparent dissociation constant (Kd) of 59 nM[1]. Robotnikinin-induced pathway activation by ShhN is inhibited by SAG (100 nM)[2]. In MDAMB231 cells, SAG (250 nM; 48 h) dramatically raises SMO mRNA and protein expression[3]. In MDAMB231 cells, SAG (250 nM; 24 and 48 hours) boosts the expression of CAXII mRNA at 24 hours under both normoxic and hypoxic conditions[3]. MDAMB231 cell migration is increased by SAG (250 nM; 24 h)[3].
ln Vivo
In CD-1 mice, SAG (1.0 mM) causes a notable rise in BV/TV at the eight-week timepoint and increased osteogenesis, primarily at the defect borders[4]. In mice, SAG (15–20 mg/kg; ip) dose-dependently causes pre-axial polydactyly to occur[5].
Animal Protocol
Animal/Disease Models: Pregnant C57BL/6J mice[5]
Doses: 15, 17, 20 mg/kg
Route of Administration: A single ip
Experimental Results: 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 at the dose of 20 mg/kg.
References

[1]. Small molecule modulation of Smoothened activity. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6.

[2]. A small molecule that binds Hedgehog and blocks its signaling in human cells. Nat Chem Biol. 2009 Mar;5(3):154-6.

[3]. Inhibition of smoothened in breast cancer cells reduces CAXII expression and cell migration. J Cell Physiol. 2018 Dec; 233(12): 9799-9811.

[4]. Combining Smoothened Agonist (SAG) and NEL-like protein-1 (NELL-1) Enhances Bone Healing. Plast Reconstr Surg. 2017 Feb 13.

[5]. 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
CAS #
2702366-44-5
Related CAS #
SAG;912545-86-9;SAG hydrochloride;2095432-58-7;(Rac)-SAG;364590-63-6
Appearance
Light yellow to light brown solid powder
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

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
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)
H2O: 100 mg/mL (177.63 mM)
DMSO: 33.33 mg/mL (59.20 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (4.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 50 mg/mL (88.81 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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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)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

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