Synonym
Monlunabant; INV-202; INV 202; INV202; (-)-MRI-1891; MRI-1891; MRI 1891; MRI1891; S-MRI-1891;
IUPAC/Chemical Name
Acetamide, N-[[[[(4S)-3-(4-chlorophenyl)-4,5-dihydro-4-phenyl-1H-pyrazol-1-yl][[[4-(trifluoromethyl)phenyl]sulfonyl]amino]methylene]amino]iminomethyl]-
InChi Key
GYJPQNPVIJXXTA-JOCHJYFZSA-N
InChi Code
InChI=1S/C26H22ClF3N6O3S/c1-16(37)32-24(31)33-25(35-40(38,39)21-13-9-19(10-14-21)26(28,29)30)36-15-22(17-5-3-2-4-6-17)23(34-36)18-7-11-20(27)12-8-18/h2-14,22H,15H2,1H3,(H3,31,32,33,35,37)/t22-/m1/s1
SMILES Code
CC(N/C(N)=N/C(N1C[C@H](C2=CC=CC=C2)C(C3=CC=C(Cl)C=C3)=N1)=N\S(C4=CC=C(C(F)(F)F)C=C4)(=O)=O)=O
Appearance
To be determined
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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
Diabetic kidney disease (DKD) is a leading cause of chronic kidney disease and affects approximately 40% of individuals with diabetes . Cases of DKD continue to rise globally as the prevalence of diabetes mellitus increases, with an estimated 415 million people living with diabetes in 2015 and a projected 642 million by 2040. DKD is associated with significant morbidity and mortality, representing 34% and 36% of all chronic kidney disease deaths in men and women, respectively. Common comorbidities including hypertension and ageing-related nephron loss further complicate disease diagnosis and progression. The progression of DKD involves several mechanisms including glomerular endothelial cell dysfunction, inflammation, and fibrosis. Targeting these mechanisms has formed the basis of several therapeutic agents. Renin-angiotensin-aldosterone system (RAAS) blockers, specifically angiotensin receptor blockers (ARBs), demonstrate significant reductions in macroalbuminuria. Sodium-glucose transporter type 2 (SGLT-2) inhibitors demonstrate kidney protection independent of diabetes control while also decreasing the incidence of cardiovascular events. Emerging agents including glucagon-like peptide 1 (GLP-1) agonists, anti-inflammatory agents like bardoxolone, and mineralocorticoid receptor antagonists show promise in mitigating DKD progression. Many novel therapies including monoclonal antibodies CSL346, lixudebart, and tozorakimab; mesenchymal stem/stromal cell infusion; and cannabinoid-1 receptor inverse agonism via INV-202 are currently in clinical trials and present opportunities for further drug development.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
591.01
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.
| 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 |
1: Ghose S, Satariano M, Korada S, Cahill T, Shah R, Raina R. Advancements in diabetic kidney disease management: integrating innovative therapies and targeted drug development. Am J Physiol Endocrinol Metab. 2024 Jun 1;326(6):E791-E806. doi: 10.1152/ajpendo.00026.2024. Epub 2024 Apr 17. PMID: 38630049.
2: Crater GD, Lalonde K, Ravenelle F, Harvey M, Després JP. Effects of CB1R inverse agonist, INV-202, in patients with features of metabolic syndrome. A randomized, placebo-controlled, double-blind phase 1b study. Diabetes Obes Metab. 2024 Feb;26(2):642-649. doi: 10.1111/dom.15353. Epub 2023 Nov 8. PMID: 37941317.
3: Jacquot L, Pointeau O, Roger-Villeboeuf C, Passilly-Degrace P, Belkaid R, Regazzoni I, Leemput J, Buch C, Demizieux L, Vergès B, Degrace P, Crater G, Jourdan T. Therapeutic potential of a novel peripherally restricted CB1R inverse agonist on the progression of diabetic nephropathy. Front Nephrol. 2023 Mar 28;3:1138416. doi: 10.3389/fneph.2023.1138416. PMID: 37675364; PMCID: PMC10479578.
