SAR-20347
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MedKoo CAT#: 407471

CAS#: 1450881-55-6

Description: SAR-20347 is a potent dual inhibitor of JAK1 and tyrosine kinase 2 (TYK2). SAR-20347 dose dependently (1 nM-10 μM) inhibited JAK1- and/or TYK2-dependent signaling from the IL-12/IL-23, IL-22, and IFN-α receptors. In vivo, TYK2 mutant mice or treatment of wild-type mice with SAR-20347 significantly reduced IL-12-induced IFN-γ production and IL-22-dependent serum amyloid A to similar extents.


Chemical Structure

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SAR-20347
CAS# 1450881-55-6

Theoretical Analysis

MedKoo Cat#: 407471
Name: SAR-20347
CAS#: 1450881-55-6
Chemical Formula: C21H18ClFN4O4
Exact Mass: 444.10
Molecular Weight: 444.847
Elemental Analysis: C, 56.70; H, 4.08; Cl, 7.97; F, 4.27; N, 12.59; O, 14.39

Price and Availability

Size Price Availability Quantity
5mg USD 90 Ready to ship
10mg USD 150 Ready to ship
25mg USD 250 Ready to ship
50mg USD 450 Ready to ship
100mg USD 750 Ready to ship
200mg USD 1350 Ready to ship
500mg USD 2850 Ready to ship
1g USD 4250 Ready to ship
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Synonym: SAR-20347; SAR 20347; SAR20347.

IUPAC/Chemical Name: 2-(2-Chloro-6-fluorophenyl)-5-[[4-(4-morpholinylcarbonyl)phenyl]amino]-4-oxazolecarboxamide

InChi Key: HEDPDFHTQKEORT-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H18ClFN4O4/c22-14-2-1-3-15(23)16(14)19-26-17(18(24)28)20(31-19)25-13-6-4-12(5-7-13)21(29)27-8-10-30-11-9-27/h1-7,25H,8-11H2,(H2,24,28)

SMILES Code: O=C(C1=C(NC2=CC=C(C(N3CCOCC3)=O)C=C2)OC(C4=C(F)C=CC=C4Cl)=N1)N

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target: SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50s of 0.6, 23, 26 and 41 nM, respectively.
In vitro activity: Because SAR-20347 inhibits TYK2 and JAK1 signaling, whether SAR-20347 blocked the development of Th1, Th2, or Th17 cells was investigated in vitro. Th1 cells require IL-12 signaling for development, a TYK2-dependent process, and Th17 cells utilize IL-6, a JAK1-dependent process. Th2 cells, which require IL-4 for development, a JAK1/3-dependent process, were also assessed. The presence of 1 μM SAR-20347 during Th17-skewing conditions reduced the percent of IL-17+cells (Figure 2A/B). Moreover, there was a dramatic increase in Foxp3+ cells (t-test, p = 0.002), an observation that is consistent with inhibition of IL-6 signaling and causing the cells to be redirected to the Treg lineage (Figure 2A). Reference: J Immunol. 2014 Oct 1;193(7):3278-87. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4170002/
In vivo activity: Treatment of TYK2 mutant mice or wild-type mice with SAR-20347 significantly reduced IL-12-induced IFN-γ production and IL-22-dependent serum amyloid A to similar extents. These results indicate that in these models, SAR-20347 is probably acting through inhibition of TYK2. Strikingly, 60 mg/kg SAR-20347 inhibited the production of IFN-γ in the serum by 91% compared to vehicle-treated animals (Supplemental Figure S1C), demonstrating that SAR-20347 can inhibit TYK2 signaling in vivo. Reference: J Immunol. 2014 Oct 1;193(7):3278-87. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4170002/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 94.5 212.43

Preparing Stock Solutions

The following data is based on the product molecular weight 444.85 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Works MG, Yin F, Yin CC, Yiu Y, Shew K, Tran TT, Dunlap N, Lam J, Mitchell T, Reader J, Stein PL, D'Andrea A. Inhibition of TYK2 and JAK1 ameliorates imiquimod-induced psoriasis-like dermatitis by inhibiting IL-22 and the IL-23/IL-17 axis. J Immunol. 2014 Oct 1;193(7):3278-87. doi: 10.4049/jimmunol.1400205. Epub 2014 Aug 25. PMID: 25156366; PMCID: PMC4170002.
In vitro protocol: 1. Works MG, Yin F, Yin CC, Yiu Y, Shew K, Tran TT, Dunlap N, Lam J, Mitchell T, Reader J, Stein PL, D'Andrea A. Inhibition of TYK2 and JAK1 ameliorates imiquimod-induced psoriasis-like dermatitis by inhibiting IL-22 and the IL-23/IL-17 axis. J Immunol. 2014 Oct 1;193(7):3278-87. doi: 10.4049/jimmunol.1400205. Epub 2014 Aug 25. PMID: 25156366; PMCID: PMC4170002.
In vivo protocol: 1. Works MG, Yin F, Yin CC, Yiu Y, Shew K, Tran TT, Dunlap N, Lam J, Mitchell T, Reader J, Stein PL, D'Andrea A. Inhibition of TYK2 and JAK1 ameliorates imiquimod-induced psoriasis-like dermatitis by inhibiting IL-22 and the IL-23/IL-17 axis. J Immunol. 2014 Oct 1;193(7):3278-87. doi: 10.4049/jimmunol.1400205. Epub 2014 Aug 25. PMID: 25156366; PMCID: PMC4170002.

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1: Works MG, Yin F, Yin CC, Yiu Y, Shew K, Tran TT, Dunlap N, Lam J, Mitchell T,
Reader J, Stein PL, D'Andrea A. Inhibition of TYK2 and JAK1 ameliorates
imiquimod-induced psoriasis-like dermatitis by inhibiting IL-22 and the
IL-23/IL-17 axis. J Immunol. 2014 Oct 1;193(7):3278-87. doi:
10.4049/jimmunol.1400205. Epub 2014 Aug 25. PubMed PMID: 25156366; PubMed Central
PMCID: PMC4170002.