Budiodarone tartrate

Product Name: Budiodarone tartrate
CAS No.: 1346623-17-3
Chemical Name: Budiodarone tartrate
Synonyms: CS-2731;CCX 168;Avacopan (CCX168);Budiodarone tartrate;Atogepant Impurity 38;Avacopan (CCX168) ，S0474;Avacopan, CCX 168, CS-2731;(2R,3S)-2-[4-(cyclopentylamino)phenyl]-1-(2-fluoro-6-methylbenzoyl)-N-[4-methyl3-(trifluoromethyl)phenyl]piperidine-3-carboxamide;3-Piperidinecarboxamide, 2-[4-(cyclopentylamino)phenyl]-1-(2-fluoro-6-methylbenzoyl)-N-[4-methyl-3-(trifluoromethyl)phenyl]-, (2R,3S)-;(S)-N-((3R,5R,6S)-6-methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)piperidin-3-yl)-2'-oxo-1',2',5,7-tetrahydrospiro[cyclopenta[b]pyridine-6,3'-pyrrolo[2,3-b]pyridine]-3-carboxamide
CBNumber: CB03159875
Molecular Formula: C33H35F4N3O2
Formula Weight: 581.64
MOL File: 1346623-17-3.mol

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Budiodarone tartrate Property

Boiling point:: 730.7±60.0 °C(Predicted)
Density: 1.287±0.06 g/cm3(Predicted)
solubility: DMF: 12 mg/ml; DMSO: 5 mg/ml; Ethanol: 3 mg/ml
form: A solid
pka: 14.02±0.70(Predicted)
color: White to off-white
InChIKey: PUKBOVABABRILL-YZNIXAGQSA-N
SMILES: C(C1C(=CC=CC=1C)F)(N1CCC[C@@H]([C@@H]1C1C=CC(=CC=1)NC1CCCC1)C(=O)NC1C=CC(=C(C=1)C(F)(F)F)C)=O

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H302Harmful if swallowed

H410Very toxic to aquatic life with long lasting effects

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P273Avoid release to the environment.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P391Collect spillage. Hazardous to the aquatic environment

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

DC Chemicals

Product number: DC11688
Product name: Avacopan
Purity: >98%
Packaging: 250mg
Price: $1300
Updated: 2021/12/16

DC Chemicals

Product number: DC11688
Product name: Avacopan
Purity: >98%
Packaging: 1g
Price: $2600
Updated: 2021/12/16

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Budiodarone tartrate Chemical Properties,Usage,Production

Uses

Avacopan (CCX168) is a potent, selective and orally available complement 5a receptor (C5aR) inhibitor with an IC50 of 0.1 nM.

in vivo

CCX168 is shown to be well tolerated across a broad dose range (1 to 100 mg) and it showed dose-dependent pharmacokinetics. An oral dose of 30 mg CCX168 given twice daily blocked the C5a-induced upregulation of CD11b in circulating neutrophils by 94% or greater throughout the entire day, demonstrating essentially complete target coverage. In mice dosed orally with 0.03 mg/kg of CCX168, the resulting plasma CCX168 concentration of 15 nM (8.7 ng/mL) reduces the drop in circulating leukocytes from 53% to 25%. In mice administered 0.3 mg/kg of CCX168, the resulting plasma CCX168 concentration of 75 nM (44 ng/mL) reduces the drop in circulating leukocytes from 53% to only 10% relative to baseline (p<0.05 for CCX168 vs. vehicle control). Oral doses of CCX168 of either 3 or 30 mg/kg completely blocks C5a-induced leukopenia in hC5aR knock-in mice^[1]. Oral CCX168, 30 mg/kg daily, reduces the severity of anti-MPO NCGN in hC5aR mice. Glomerular crescents are reduced from 30.4% to 3.3% with CCX168. Urine hematuria, proteinuria, and leukocyturia are reduced in mice receiving CCX168, 30 mg/kg per day. The protection by CCX168 results in reduced crescents and necrosis^[2].

References

[1] Bekker P, et al. Characterization of Pharmacologic and Pharmacokinetic Properties of CCX168, a Potent and Selective Orally Administered Complement 5a Receptor Inhibitor, Based on Preclinical Evaluation and Randomized Phase 1 Clinical Study. PLoS One. 2016 Oct 21;11(10):e0164646. DOI:10.1371/journal.pone.0164646
[2] Xiao H, et al. C5a receptor (CD88) blockade protects against MPO-ANCA GN. J Am Soc Nephrol. 2014 Feb;25(2):225-31. DOI:10.1681/ASN.2013020143

Budiodarone tartrate Preparation Products And Raw materials

Raw materials

Preparation Products

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Budiodarone tartrate Suppliers

China 68 United States 6 Global 74

ShangHai ChuanQian Chemcial Technique Centre

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Budiodarone tartrate

CCX 168

CS-2731

Avacopan (CCX168)

(2R,3S)-2-[4-(cyclopentylamino)phenyl]-1-(2-fluoro-6-methylbenzoyl)-N-[4-methyl3-(trifluoromethyl)phenyl]piperidine-3-carboxamide

3-Piperidinecarboxamide, 2-[4-(cyclopentylamino)phenyl]-1-(2-fluoro-6-methylbenzoyl)-N-[4-methyl-3-(trifluoromethyl)phenyl]-, (2R,3S)-

(S)-N-((3R,5R,6S)-6-methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)piperidin-3-yl)-2'-oxo-1',2',5,7-tetrahydrospiro[cyclopenta[b]pyridine-6,3'-pyrrolo[2,3-b]pyridine]-3-carboxamide

Avacopan, CCX 168, CS-2731

Atogepant Impurity 38

Avacopan (CCX168) ，S0474

1346623-17-3

C33H35F4N3O2