SAG dihydrochloride

Name: SAG dihydrochloride
Brand: MedChemExpress
SKU: HY-12848C
Rating: 5.0 (24 reviews)

Cat. No.: HY-12848C Purity: 99.56%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

SAG dihydrochloride is a potent Smoothened (Smo) receptor agonist (EC₅₀=3 nM; K_d=59 nM). SAG dihydrochloride activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo.

For research use only. We do not sell to patients.

SAG dihydrochloride Chemical Structure

CAS No. : 2702366-44-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 291	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 291	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 75	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 490	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 24 publication(s) in Google Scholar

Other Forms of SAG dihydrochloride:

SAG In-stock
SAG hydrochloride In-stock
(Rac)-SAG Get quote

23 Publications Citing Use of MCE SAG dihydrochloride

: SAG dihydrochloride purchased from MedChemExpress. Usage Cited in: Development. 2018 Sep 20;145(18). pii: dev164830. [Abstract]; WT MEF cells are treated with 100 nM SAG, 0.1mM ATP, or 0.1mM NHATP for 10 min (U). p-Creb, total Creb and Tubulin protein levels are detected by Western blotting.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

EC50: 3 nM (Smo)^[1]

In Vitro

SAG (0.1 nM-100 μM; 30 h) induces firefly luciferase expression in Shh-LIGHT2 cells with an EC₅₀ of 3 nM and then inhibits expression at higher concentrations^[1].
SAG (1-1000 nM; 1 h) competes for the binding of BODIPY-cyclopamine to Smo-expressing Cos-1 cells, yielding an apparent dissociation constant (K_d) of 59 nM for the SAG/Smo complex^[1].
SAG (100 nM) inhibits the inhibitory effect of ShhN-induced pathway activation by Robotnikinin^[2].
SAG (250 nM; 48 h) significantly increases SMO mRNA and protein expression in MDAMB231 cells^[3].
SAG (250 nM; 24 and 48 h) increases CAXII mRNA expression in MDAMB231 cells at 24h in normoxic and hypoxic conditions in MDAMB231 cells^[3].
SAG (250 nM; 24 h) increases MDAMB231 cells migration^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SAG (1.0 mM) induces more osteogenesis mainly at the defect borders and a significant increase in BV/TV at the eight week timepoint in CD-1 mice^[4].
SAG (15-20 mg/kg; i.p.) induces pre-axial polydactyly prevalently in a dose-dependent manner in mice^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Pregnant C57BL/6J mice^[5]
Dosage:	15, 17, 20 mg/kg
Administration:	A single i.p.
Result:	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.

Molecular Weight

562.98

Formula

C₂₈H₃₀Cl₃N₃OS

CAS No.

2702366-44-5

Appearance

Solid

Color

Light yellow to light brown

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.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (177.63 mM; Need ultrasonic)

DMSO : 33.33 mg/mL (59.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7763 mL	8.8813 mL	17.7626 mL
5 mM	0.3553 mL	1.7763 mL	3.5525 mL
10 mM	0.1776 mL	0.8881 mL	1.7763 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 50 mg/mL (88.81 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.56%

Select Batch:

Data Sheet (281 KB) SDS (252 KB)

COA (252 KB) LCMS (273 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

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

[4]. Lee S, et al. Combining Smoothened Agonist (SAG) and NEL-like protein-1 (NELL-1) Enhances Bone Healing. Plast Reconstr Surg. 2017 Feb 13. [Content Brief]

[5]. 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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	1.7763 mL	8.8813 mL	17.7626 mL	44.4066 mL
	5 mM	0.3553 mL	1.7763 mL	3.5525 mL	8.8813 mL
	10 mM	0.1776 mL	0.8881 mL	1.7763 mL	4.4407 mL
	15 mM	0.1184 mL	0.5921 mL	1.1842 mL	2.9604 mL
	20 mM	0.0888 mL	0.4441 mL	0.8881 mL	2.2203 mL
	25 mM	0.0711 mL	0.3553 mL	0.7105 mL	1.7763 mL
	30 mM	0.0592 mL	0.2960 mL	0.5921 mL	1.4802 mL
	40 mM	0.0444 mL	0.2220 mL	0.4441 mL	1.1102 mL
	50 mM	0.0355 mL	0.1776 mL	0.3553 mL	0.8881 mL
H₂O	60 mM	0.0296 mL	0.1480 mL	0.2960 mL	0.7401 mL
	80 mM	0.0222 mL	0.1110 mL	0.2220 mL	0.5551 mL
	100 mM	0.0178 mL	0.0888 mL	0.1776 mL	0.4441 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.