R-GNE-140 free base · Synonyms: (R)-GNE-140
-GNE-140 is a potent lactate dehydrogenase A inhibitor.
For research use only. Not for human or veterinary use.
R-GNE-140 structure
CAS No.: 2003234-63-5
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 100 mg | USD 540.00 | BP-02325-100mg | In stock | Get quote |
| 250 mg | USD 1,080.00 | BP-02325-250mg | In stock | Get quote |
| 500 mg | USD 1,728.00 | BP-02325-500mg | In stock | Get quote |
| 1 g | USD 2,765.00 | BP-02325-1g | In stock | Get quote |
| 2 g | USD 4,423.00 | BP-02325-2g | In stock | Get quote |
| 3 g | USD 5,300.00 | BP-02325-3g | In stock | Get quote |
Need another size or custom synthesis? Request a quote.
Description
(R)-GNE-140 is a potent lactate dehydrogenase A (LDHA) inhibitor, with IC50s of 3 nM and 5 nM for LDHA and LDHB, respectively; (R)-GNE-140 is 18-fold more potent than S enantiomer.
Biological activity
In Vitro (R)-GNE-140 (10 μM; 48 h) reduces intracellular lactate levels, decreases the surface area of neonatal mouse cardiomyocytes, downregulates the expression of cardiac hypertrophy markers, and inhibits multiple histone lysine lactylation modifications, thereby alleviating angiotensin II (Ang II)-induced hypertrophy of neonatal mouse cardiomyocytes (NMCM). Pretreatment of mouse RAW264.7 macrophages with (R)-GNE-140 (10 μM; 4 h) inhibits PM2.5-induced glycolysis, histone lactylation, pro-fibrotic gene expression and cytokine secretion, and partially reverses macrophage-mediated epithelial-mesenchymal transition (EMT) in MLE-12 cells. (R)-GNE-140 (6-12 h) inhibits MSM-induced Arg1 mRNA expression in MRSA-infected THP1 cells at 6 h and 12 h post-infection. (R)-GNE-140 (6-12 h) blocks MSM-induced Arg1 protein expression in THP1 cells infected with MRSA at 6 h and 12 h post-infection. (R)-GNE-140 (Compound 29-R) can inhibit lactate production in human pancreatic cancer MiaPaca2 cells, with its IC50 being 0.67 μM. In Vivo (R)-GNE-140 (5 mg/kg; i.t.; once every other day; 4 weeks) reduces PM2.5-induced pulmonary inflammation and fibrosis in male C57BL/6 J mice by inhibiting glycolysis and subsequent histone lactylation.
Identifiers
- SMILES
-
OC1=C(SC2=CC=CC=C2Cl)C(=O)N[C@@](C1)(C1=CSC=C1)C1=CC=C(C=C1)N1CCOCC1 - InChIKey
-
SUFXXEIVBZJOAP-RUZDIDTESA-N
Specifications
- MW (average)
- 499.0450
- Formula
- C25H23ClN2O3S2
- CAS No.
- 2003234-63-5
- Physical state
- Solid
- Color
- Off-white to yellow
- Shipping
- 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
- Powder -20℃ 2 years; In solvent -20℃ 1 month;
Solubility
soluble in DMSO