BR102910 is a selective fibroblast activation protein (FAP) inhibitor (antagonist) with IC50 of 2 nM. BR102910 also inhibits prolyl oligopeptidase (PREP) with IC50 of 49.00 μM. BR102910 may be utilized in type 2 diabetes research.

Physicochemical Properties

Molecular Formula	C18H14CL2F2N4O2S
Molecular Weight	459.297167301178
Exact Mass	458.018
CAS #	2505339-54-6
PubChem CID	155754825
Appearance	White to off-white solid powder
LogP	3.9
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	5
Heavy Atom Count	29
Complexity	692
Defined Atom Stereocenter Count	1
SMILES	ClC1=C(C=CC(=C1)CC1=NC(=CS1)C(NCC(N1CC(CC1C#N)(F)F)=O)=O)Cl
InChi Key	JTSUDVSZJDOOJG-NSHDSACASA-N
InChi Code	InChI=1S/C18H14Cl2F2N4O2S/c19-12-2-1-10(3-13(12)20)4-15-25-14(8-29-15)17(28)24-7-16(27)26-9-18(21,22)5-11(26)6-23/h1-3,8,11H,4-5,7,9H2,(H,24,28)/t11-/m0/s1
Chemical Name	N-[2-[(2S)-2-cyano-4,4-difluoropyrrolidin-1-yl]-2-oxoethyl]-2-[(3,4-dichlorophenyl)methyl]-1,3-thiazole-4-carboxamide
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 (e.g. under nitrogen), avoid exposure to moisture and light.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vivo	In a dose-dependent manner, BR102910 (C57BL/6J mice, 0-30 mg/kg, po, once) exhibits a substantial suppression of FAP [1].
Animal Protocol	Animal/Disease Models: C57BL/6J mice (n = 5 per group) [1] Doses: 0, 10 and 30 mg/kg Route of Administration: Orally, once Experimental Results: Demonstrated significant FAP inhibition in a dose-dependent manner effect.
References	[1]. Identification of BR102910 as a selective fibroblast activation protein (FAP) inhibitor. Bioorg Med Chem Lett. 2021 Apr 1;37:127846.

Solubility Data

Solubility (In Vitro)

DMSO : ~100 mg/mL (~217.72 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.44 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.44 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.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.1772 mL	10.8861 mL	21.7723 mL
	5 mM	0.4354 mL	2.1772 mL	4.3545 mL
	10 mM	0.2177 mL	1.0886 mL	2.1772 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.