Product Name :
IMT1B
Description:
IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects.
CAS:
2304621-06-3
Molecular Weight:
473.88
Formula:
C24H21ClFNO6
Chemical Name:
(3S)-1-[(2R)-2-{[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-chromen-7-yl]oxy}propanoyl]piperidine-3-carboxylic acid
Smiles :
C[C@@H](OC1=CC=C2C(=C1)OC(=O)C=C2C1=CC=C(F)C=C1Cl)C(=O)N1C[C@H](CCC1)C(O)=O
InChiKey:
PFEKWBKJUBCXDT-KGLIPLIRSA-N
InChi :
InChI=1S/C24H21ClFNO6/c1-13(23(29)27-8-2-3-14(12-27)24(30)31)32-16-5-7-18-19(11-22(28)33-21(18)10-16)17-6-4-15(26)9-20(17)25/h4-7,9-11,13-14H,2-3,8,12H2,1H3,(H,30,31)/t13-,14+/m1/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects.|Product information|CAS Number: 2304621-06-3|Molecular Weight: 473.88|Formula: C24H21ClFNO6|Chemical Name: (3S)-1-[(2R)-2-{[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-chromen-7-yl]oxy}propanoyl]piperidine-3-carboxylic acid|Smiles: C[C@@H](OC1=CC=C2C(=C1)OC(=O)C=C2C1=CC=C(F)C=C1Cl)C(=O)N1C[C@H](CCC1)C(O)=O|InChiKey: PFEKWBKJUBCXDT-KGLIPLIRSA-N|InChi: InChI=1S/C24H21ClFNO6/c1-13(23(29)27-8-2-3-14(12-27)24(30)31)32-16-5-7-18-19(11-22(28)33-21(18)10-16)17-6-4-15(26)9-20(17)25/h4-7,9-11,13-14H,2-3,8,12H2,1H3,(H,30,31)/t13-,14+/m1/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 250 mg/mL (527.Oleic acid 56 mM; Need ultrasonic).Epirubicin hydrochloride |Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.PMID:23773119 |Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|IMT1B is a noncompetitive inhibitor that causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro. IMT1B (0.01 nM-10 μM; 72-168 hours) dose-dependently decreases in cell viability in A2780, A549 and HeLa cells. IMT1B depletes cellular metabolites. IMT1B increases the levels of mono- and diphosphate nucleotides that results in a considerable increase in the AMP/ATP ratio and levels of phosphorylated AMPK.|In Vivo:|IMT1B (100 mg/kg; p.o.; daily; for four weeks) significantly reduces tumour size in mice containing xenografts. IMT1B reduces mtDNA transcript levels and respiratory-chain subunit levels in tumours. IMT1B exhibits good oral bioavailability (mice 101 %) and Cmax (mice 5149 ng/mL) following oral administration (mice 10 mg/kg). IMT1B exhibits elimination half-life (mice 1.88 h) due to plasma clearance (mice 0.44 L/h/kg) following intravenous administration (mice 1 mg/kg).|Products are for research use only. Not for human use.|