[CAS NO. 2702366-44-5]  SAGdihydrochloride

Ships within Stock Price Qty Total
$0.00
$0.00
Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis
request a quote
If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [2702366-44-5]

Distributor
Catalog
HY-12848C
Brand
MCE
CAS
2702366-44-5

DESCRIPTION [2702366-44-5]

Overview

MDL-
Molecular Weight562.98
Molecular FormulaC28H30Cl3N3OS
SMILESO=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

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


Summary

SAG dihydrochloride is a potent Smoothened (Smo) receptor agonist ( EC 50 =3 nM; K d =59 nM). SAG dihydrochloride activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo [1] [2] [3] .


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 EC 50 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] .

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] .

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.

Appearance

Solid


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:

H 2 O : 100 mg/mL ( 177.63 mM ; Need ultrasonic)

DMSO : 33.33 mg/mL ( 59.20 mM ; Need ultrasonic)

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
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: PBS

    Solubility: 50 mg/mL (88.81 mM); Clear solution; Need ultrasonic

  • 2.

    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

  • 3.

    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

  • 4.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

* All of the co-solvents are available by MCE.