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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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L649733-1mg | 1mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $261.90 | |
L649733-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $550.90 | |
L649733-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $850.90 | |
L649733-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,750.90 |
Specifications & Purity | ≥99% |
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Biochemical and Physiological Mechanisms | LDH-IN-1 is a novel pyrazole-based inhibitor of human lactate dehydrogenase (LDH) with IC 50 s of 32 and 27 nM for LDHA and LDHB, respectively. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | LDH-IN-1 is a novel pyrazole-based inhibitor of human lactate dehydrogenase (LDH) with IC 50 s of 32 and 27 nM for LDHA and LDHB, respectively. In Vitro LDH-IN-1 exhibits low nM inhibition of both LDHA and LDHB (IC 50 =32, 27 nM, respectively), submicromolar inhibition of lactate production, and inhibition of lactate in MiaPaCa2 pancreatic cancer and A673 sarcoma cells (IC 50 =0.517, 0.854μM, respectively). LDH-IN-1 inhibits the growth of MiaPaCa2 pancreatic cancer and A673 sarcoma cells with IC 50 s of 2.23 and 1.21 μM). Dose?response treatment of MiaPaCa-2 cells with LDH-IN-1 shows effects on cellular proliferation at concentrations as low as 250 nM and with nearly complete arrest of cell growth at 20 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo LDH-IN-1 shows clearance values that far exceed hepatic blood flow (HBF) in mouse species (90 mL/min/kg), with in vivo clearances of 227 mL/min/kg . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 32 nM (LDHA), 27 nM (LDHB) |
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IUPAC Name | 2-[5-(cyclopropylmethyl)-3-(3-phenylphenyl)-4-[(4-sulfamoylphenyl)methyl]pyrazol-1-yl]-1,3-thiazole-4-carboxylic acid |
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INCHI | InChI=1S/C30H26N4O4S2/c31-40(37,38)24-13-11-19(12-14-24)15-25-27(16-20-9-10-20)34(30-32-26(18-39-30)29(35)36)33-28(25)23-8-4-7-22(17-23)21-5-2-1-3-6-21/h1-8,11-14,17-18,20H,9-10,15-16H2,(H,35,36)(H2,31,37,38) |
InChi Key | ALJORCZKMBZYCR-UHFFFAOYSA-N |
Canonical SMILES | C1CC1CC2=C(C(=NN2C3=NC(=CS3)C(=O)O)C4=CC=CC(=C4)C5=CC=CC=C5)CC6=CC=C(C=C6)S(=O)(=O)N |
Isomeric SMILES | C1CC1CC2=C(C(=NN2C3=NC(=CS3)C(=O)O)C4=CC=CC(=C4)C5=CC=CC=C5)CC6=CC=C(C=C6)S(=O)(=O)N |
PubChem CID | 131955127 |
Molecular Weight | 570.68 |
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Solubility | DMSO : 52 mg/mL (91.12 mM; Need ultrasonic) |
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