Free shipping on all orders over $ 500

SAR247799

Cat. No. M21193
SAR247799 Structure
Synonym:

S1P1 agonist 3

Size Price Availability
Free Delivery on orders over USD 500 Bulk Inquiry?
Quality Control & Documentation
Biological Activity

The S1P1 agonist SAR247799 is a biased agonist of the S1P1 sphingosine receptor, preferentially activating G protein signaling over the β-arrestin and internalization pathways.

Chemical Information
Molecular Weight 425.82
Formula C21H16ClN3O5
CAS Number 1315311-14-8
Form Solid
Solubility (25°C) DMSO 33.33 mg/mL
Storage -20°C
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Maria Francesca Evaristi, et al. PLoS One. A G-protein-biased S1P1 agonist, SAR247799, improved LVH and diastolic function in a rat model of metabolic syndrome

[2] Luc Bergougnan, et al. Br J Clin Pharmacol. Endothelial-protective effects of a G-protein-biased sphingosine-1 phosphate receptor-1 agonist, SAR247799, in type-2 diabetes rats and a randomized placebo-controlled patient trial

[3] Patrick Grailhe, et al. FEBS Open Bio. A label-free impedance assay in endothelial cells differentiates the activation and desensitization properties of clinical S1P1 agonists

[4] Luc Bergougnan, et al. Br J Clin Pharmacol. First-in-human study of the safety, tolerability, pharmacokinetics and pharmacodynamics of single and multiple oral doses of SAR247799, a selective G-protein-biased sphingosine-1 phosphate receptor-1 agonist for endothelial protection

[5] Bruno Poirier, et al. Sci Signal. A G protein-biased S1P1 agonist, SAR247799, protects endothelial cells without affecting lymphocyte numbers

Related S1P Receptor Products
VTX-002

VTX-002 is an orally active, selective S1P receptor 1 modulator for studies related to ulcerative colitis.
TRV045

TRV045 is an S1P receptor modulator that can be used in studies related to central nervous system disorders.
S1PR1 modulator 1 

S1PR1 modulator 1 is a selective S1PR1 inhibitor, with a pIC50 of 7.6, with >40- and >80-fold selectivity, over the other S1PR isoforms S1PR2/3/4.
Ozanimod hydrochloride

Ozanimod (RPC-1063) hydrochloride, a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod hydrochloride has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod hydrochloride can be used for the research of relapsing multiple sclerosis (MS) .
Icanbelimod

Icanbelimod (S1p receptor agonist 1) is a potent and orally active S1P1 receptor agonist, exhibits an activity of inducing S1P1 internalization (EC50=9.83 nM). Icanbelimod has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis).
  Catalog
Abmole Inhibitor Catalog




Keywords: SAR247799, S1P1 agonist 3 supplier, S1P Receptor, inhibitors, activators

 
Get to Know Us
Customer Support
Resources
Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.