ChemicalBook > CAS DataBase List > 3-Piperidinecarboxylic acid, 1-[(2R)-2-[[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-, (3S)-

3-Piperidinecarboxylic acid, 1-[(2R)-2-[[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-, (3S)-

Product Name
3-Piperidinecarboxylic acid, 1-[(2R)-2-[[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-, (3S)-
CAS No.
2304621-06-3
Chemical Name
3-Piperidinecarboxylic acid, 1-[(2R)-2-[[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-, (3S)-
Synonyms
IMT1B (LDC203974);IMT1B, 10 mM in DMSO;(S)-1-((R)-2-(4-(2-chloro-4-fluorophenyl)-2-oxo-2H-chromen-7-yloxy)propanoyl)piperidine-3-carboxylic acid;(3S)-1-[(2R)-2-[[4-(2-Chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-3-piperidinecarboxylic acid;3-Piperidinecarboxylic acid, 1-[(2R)-2-[[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-, (3S)-;Inhibitor,inhibit,POLRMT,oxidative,IMT-1B,LDC-203974,human,LDC 203974,anti-tumour,mtDNA,phosphorylation,IMT1B,OXPHOS,RNA,mitochondrial,DNA,polymerase
CBNumber
CB78218435
Molecular Formula
C24H21ClFNO6
Formula Weight
473.88
MOL File
2304621-06-3.mol
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3-Piperidinecarboxylic acid, 1-[(2R)-2-[[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-, (3S)- Property

Boiling point:
705.7±60.0 °C(Predicted)
Density 
1.426±0.06 g/cm3(Predicted)
pka
4.33±0.20(Predicted)
form 
Solid
color 
White to off-white
InChIKey
PFEKWBKJUBCXDT-KGLIPLIRSA-N
SMILES
N1(C(=O)[C@H](OC2=CC=C3C(=C2)OC(=O)C=C3C2=CC=C(F)C=C2Cl)C)CCC[C@H](C(O)=O)C1
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

DC Chemicals
Product number
025860
Product name
LDC203974(IMT1B)
Packaging
001
Price
$480
Updated
2021/12/16
DC Chemicals
Product number
025860
Product name
LDC203974(IMT1B)
Packaging
002
Price
$850
Updated
2021/12/16
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3-Piperidinecarboxylic acid, 1-[(2R)-2-[[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-, (3S)- Chemical Properties,Usage,Production

Uses

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[1].

in vivo

IMT1B (100 mg/kg; p.o.; daily; for four weeks) significantly reduces tumour size in mice containing xenografts[1].
IMT1B reduces mtDNA transcript levels and respiratory-chain subunit levels in tumours[1].
IMT1B exhibits good oral bioavailability (mice 101 %) and Cmax (mice 5149 ng/mL) following oral administration (mice 10 mg/kg)[1].
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)[1].

Animal Model:7-9 weeks female BALB/c nude mice, with A2780 cells xenograft[1]
Dosage:100 mg/kg
Administration:Oral administration, daily, for four weeks
Result:Led to a clear reduction of tumour volume.
Animal Model:Mice[1]
Dosage:1 mg/kg for i.v.; 10 mg/kg for oral (Pharmacokinetic Analysis)
Administration:Intravenous administration and oral administration
Result:Oral bioavailability (101%), Cmax (5149 ng/mL), T1/2 (1.88 h).

References

[1] Nina A Bonekamp, et al. Small-molecule inhibitors of human mitochondrial DNA transcription. Nature. 2020 Dec;588(7839):712-716. DOI:10.1038/s41586-020-03048-z

3-Piperidinecarboxylic acid, 1-[(2R)-2-[[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-, (3S)- Preparation Products And Raw materials

Raw materials

Preparation Products

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3-Piperidinecarboxylic acid, 1-[(2R)-2-[[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-, (3S)- Suppliers

China 32 United States 2 Global 34
Anhui JYHX CO., LTD.
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2304621-06-3, 3-Piperidinecarboxylic acid, 1-[(2R)-2-[[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-, (3S)-Related Search:


  • 3-Piperidinecarboxylic acid, 1-[(2R)-2-[[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-, (3S)-
  • (S)-1-((R)-2-(4-(2-chloro-4-fluorophenyl)-2-oxo-2H-chromen-7-yloxy)propanoyl)piperidine-3-carboxylic acid
  • Inhibitor,inhibit,POLRMT,oxidative,IMT-1B,LDC-203974,human,LDC 203974,anti-tumour,mtDNA,phosphorylation,IMT1B,OXPHOS,RNA,mitochondrial,DNA,polymerase
  • (3S)-1-[(2R)-2-[[4-(2-Chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-3-piperidinecarboxylic acid
  • IMT1B (LDC203974)
  • IMT1B, 10 mM in DMSO
  • 2304621-06-3
  • C24H21ClFNO6