Shanghai Jizhi Biochemical Technology Co., Ltd
China
Product Name: Darunavir Ethanolate
Price: ￥586.0/5mg ￥3216.0/50mg ￥1076.0/10mg ￥1866.0/25mg
Purity: 98.0%
Stocking Period: 2 Day
Contact: Liu jia

DC Chemicals Limited
China
Product Name: Darunavir ethanolate
Price: $300.0/100mg $600.0/250mg $1200.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: Darunavir ethanolate
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

Zhejiang Hangyu API Co., Ltd
China
Product Name: Darunavir Ethanolate
Price: ￥Inquiry/1kg
Purity: 99.5%
Stocking Period: Inquiry
Contact: Vinnie

Henan Tianfu Chemical Co., Ltd.
China
Product Name: [14C]-Darunavir ethanolate
Price: $Inquiry/1kg $Inquiry/25kg $Inquiry/1000kg $Inquiry/10ton
Purity: 99.0%
Stocking Period: Inquiry
Contact: Anson

635728-49-3

635728-49-3 structure

635728-49-3 structure

Name: Darunavir Ethanolate
Chemical Name: [14C]-Darunavir ethanolate
CAS Number: 635728-49-3
Molecular Formula: C₂₉H₄₃N₃O₈S
Molecular Weight: 593.732
Catalog: Biochemical Inhibitor Proteases HIV Protease Inhibitor
Create Date: 2018-02-14 08:00:00
Modify Date: 2024-01-03 16:57:06
Darunavir ethanolate (TMC114 ethanolate) is a potent HIV protease inhibitor used to treat and prevent HIV/AIDS. Darunavir has a Ki of 1 nM for wild type HIV-1 protease.

Name	[14C]-Darunavir ethanolate
Synonyms	DARUNAVIR ETHANOLATE(PREZISTA) TMC114 (3R,3aS,6aR)-Hexahydrofuro[2,3-b]fur-3-yl-[(1S,2R)-3-{[(4-aminophenyl)sulfonyl](2-methylpropyl)amino}-1-benzyl-2-hydroxypropyl]carbamat-ethanol(1:1) (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl [(1S,2R)-3-{[(4-aminophenyl)sulfonyl](2-methylpropyl)amino}-1-benzyl-2-hydroxypropyl]carbamate - ethanol (1:1) [(1S,2R)-3-{[(4-aminophényl)sulfonyl](2-méthylpropyl)amino}-1-benzyl-2-hydroxypropyl]carbamate de (3R,3aS,6aR)-hexahydrofuro[2,3-b]fur-3-yle - éthanol (1:1) Darunavir Ethanolate (3R,3aS,6aR)-Hexahydrofuro[2,3-b]furan-3-yl [(2S,3R)-4-{[(4-aminophenyl)sulfonyl](isobutyl)amino}-3-hydroxy-1-phenyl-2-butanyl]carbamate - ethanol (1:1) Carbamic acid, N-[(1S,2R)-3-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]-, (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester, compd. with ethanol (1:1) carbamic acid, [(1S,2R)-3-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]-, (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester, compd. with ethanol (1:1) UNII-33O78XF0BW Darunavir Ethanolate(Prezista) Darunavir (Ethanolate) DARUNAVIR THANOLATE

Description	Darunavir ethanolate (TMC114 ethanolate) is a potent HIV protease inhibitor used to treat and prevent HIV/AIDS. Darunavir has a Ki of 1 nM for wild type HIV-1 protease.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> HIV Protease Signaling Pathways >> Anti-infection >> HIV Research Areas >> Infection
Target	Ki: 1 nM (WT HIV-1 protease)[1]
In Vitro	Darunavir is a broad-spectrum potent inhibitor active against HIV-1 clinical isolates with minimal cytotoxicity. Darunavir forms hydrogen bonds with the conserved main-chain atoms of Asp29 and Asp30 of the protease. These interactions are proposed to be critical for the potency of this compound against HIV isolates that are resistant to multiple protease inhibitors[1]. In an in vitro study in MT-2 cells, the potency of darunavir is greater than that of saquinavir, amprenavir, nelfinavir, indinavir, lopinavir and ritonavir. Darunavir is primarily metabolized by the hepatic cytochrome P450 (CYP) enzymes, primarily CYP3A. The ‘boosting’ dose of ritonavir acts an an inhibitor of CYP3A, thereby increasing darunavir bioavailability[2].
In Vivo	Darunavir is effective against wild-type and PI-resistant HIV, and has an oral bioavailability of 37%. It needs to be combined with ritonavir, which increases the bioavailability to 82%[3].
References	[1]. Tie Y, et al. High resolution crystal structures of HIV-1 protease with a potent non-peptide inhibitor (UIC-94017) active against multi-drug-resistant clinical strains. J Mol Biol. 2004 Apr 23;338(2):341-52. [2]. McKeage K, et al. Darunavir: a review of its use in the management of HIV infection in adults. Drugs. 2009;69(4):477-503. [3]. Bhalekar MR, et al. In-vivo bioavailability and lymphatic uptake evaluation of lipid nanoparticulates of darunavir. Drug Deliv. 2016 Sep;23(7):2581-2586.

Molecular Formula	C₂₉H₄₃N₃O₈S
Molecular Weight	593.732
Exact Mass	593.277100
PSA	169.03000
LogP	4.42680
Storage condition	-20℃

HS Code	29334900

98818-34-9 structure

98818-34-9

~%

635728-49-3 structure

635728-49-3

Literature: Vellanki, Siva Rama Prasad; Sahu, Arabinda; Katukuri, Aravind Kumar; Vanama, Vikram; Kothari, Satishbabu; Ponnekanti, Venkata Suryanarayana; Datta, Debashish Patent: US2012/251826 A1, 2012 ;

64-17-5 structure

64-17-5

192725-55-6 structure

192725-55-6

169280-56-2 structure

169280-56-2

~83%

635728-49-3 structure

635728-49-3

Literature: Vellanki, Siva Rama Prasad; Sahu, Arabinda; Katukuri, Aravind Kumar; Vanama, Vikram; Kothari, Satishbabu; Ponnekanti, Venkata Suryanarayana; Datta, Debashish Patent: US2012/251826 A1, 2012 ; Location in patent: Page/Page column 10 ;

98760-08-8 structure

98760-08-8

~%

635728-49-3 structure

635728-49-3

Literature: US2012/251826 A1, ;

191226-98-9 structure

191226-98-9

~%

635728-49-3 structure

635728-49-3

Literature: US2012/251826 A1, ;

160232-08-6 structure

160232-08-6

~%

635728-49-3 structure

635728-49-3

Literature: US2012/251826 A1, ;

183004-94-6 structure

183004-94-6

~%

635728-49-3 structure

635728-49-3

Literature: US2012/251826 A1, ;

Precursor 7
64-17-5 169280-56-2 98760-08-8 191226-98-9
160232-08-6 183004-94-6 98818-34-9
DownStream 0