2252493-33-5

2252493-33-5 structure
2252493-33-5 structure
  • Name: (R)-ND-336
  • Chemical Name: (R)-ND-336
  • CAS Number: 2252493-33-5
  • Molecular Formula: C16H18ClNO3S2
  • Molecular Weight: 371.90
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease MMP
  • Create Date: 2020-08-09 11:46:23
  • Modify Date: 2024-01-08 17:06:12
  • (R)-ND-336 is a potent and selective MMP-9 inhibitor with a Ki of 19 nM. (R)-ND-336 inhibits MMP-2 (Ki=127 nM) and MMP-14 (Ki=119 nM). (R)-ND-336 has the potential for diabetic foot ulcers (DFUs) research[1].

Name (R)-ND-336
Description (R)-ND-336 is a potent and selective MMP-9 inhibitor with a Ki of 19 nM. (R)-ND-336 inhibits MMP-2 (Ki=127 nM) and MMP-14 (Ki=119 nM). (R)-ND-336 has the potential for diabetic foot ulcers (DFUs) research[1].
Related Catalog
Target

MMP-9:19 nM (Ki)

MMP-2:127 nM (Ki)

MMP-14:119 nM (Ki)

In Vitro (R)-ND-336 poorly inhibits other MMPs (Ki>100 μM). (R)-ND-336 has a long residence time (the time the inhibitor is bound to MMP-9, calculated as 1/koff) of 300 min[1]. A favorable IC50value of 143 μM afforded a therapeutic index (IC50/Ki for MMP-9) ratio of 7530, indicating that (R)-ND-336 is not cytotoxic[1].
In Vivo (R)-ND-336 (50 μg/wound/day for 14 days) accelerates wound healing faster[1]. (R)-ND-336 has an AUC of 1.3 μM•min after topical administration and 35 μM•min following intravenous dosing, for an AUCtop/AUCiv ratio of 3.7%, indicating minimal absorption after topical administration in db/db mice[1]. Animal Model: Female db/db mice (BKS.Cg-Dock7m+/+Leprdb/J, 8-weeks old, ∼40 g body weight)[1] Dosage: 50 μg Administration: Wound; once a day for 14 days Result: Accelerated wound healing faster and showed complete inhibition of MMP-9.
References

[1]. Trung T Nguyen, et al. Validation of Matrix Metalloproteinase-9 (MMP-9) as a Novel Target for Treatment of Diabetic Foot Ulcers in Humans and Discovery of a Potent and Selective Small-Molecule MMP-9 Inhibitor That Accelerates Healing. J Med Chem. 2018 Oct 11;61(19):8825-8837.

Molecular Formula C16H18ClNO3S2
Molecular Weight 371.90