178870-32-1|UC-781|N-(4-chloro-3-((3-methylbut-2-en-1-yl)oxy)phenyl)-2-methylfuran-3-carbothioamide|-范德生物科技公司

UC-781

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names：
N-(4-chloro-3-((3-methylbut-2-en-1-yl)oxy)phenyl)-2-methylfuran-3-carbothioamide
CAS号：
178870-32-1
MDL Number：
MF(分子式)： C17H18ClNO2S MW(分子量)： 335.846
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文别名	N-(4-chloro-3-((3-methylbut-2-en-1-yl)oxy)phenyl)-2-methylfuran-3-carbothioamide
英文别名	UC-781, UC781, UC 781
CAS号	178870-32-1
Inchi	InChI=1S/C17H18ClNO2S/c1-11(2)6-8-21-16-10-13(4-5-15(16)18)19-17(22)14-7-9-20-12(14)3/h4-7,9-10H,8H2,1-3H3,(H,19,22)
InchiKey	YZHIXLCGPOTQNB-UHFFFAOYSA-N
分子式 Formula	C17H18ClNO2S
分子量 Molecular Weight	335.846
溶解度Solubility
性状	Solid powder
储藏条件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

产品说明	UC-781(CAS:178870-32-1):仅限应用于工业或者科学研究过程中非医疗目的，不应用于人类或动物的临床诊断以及治过程疗，该产品非药用，非食用。
Introduction	UC-781 is a non-nucleoside reverse transcriptase inhibitor potenially for the treatment of HIV infection. In human cervical explant cultures, UC-781 was not only able to inhibit direct infection of mucosal tissue but was able to prevent dissemination of virus by migratory cells. UC-781 formulated into a carbopol gel (0.1%) retained significant activity against both direct tissue infection and transinfection mediated by migratory cells. Furthermore, UC-781 demonstrated prolonged inhibitory effects able to prevent both localized and disseminated infections up to 6 days post compound treatment.
Application1
Application2
Application3

警示图
危险性	Warning
危险性警示
安全声明
安全防护
备注

[1]McConville C, Friend D. Development and characterisation of a self-microemulsifying drug delivery systems (SMEDDSs) for the vaginal administration of the antiretroviral UC-78[1]Eur J Pharm Biopharm. 2013 Apr;83(3):322-9. doi: 10.1016/j.ejpb.2012.10.007. PubMed PMID: 23159711.

[2]Rezk NL. Development and validation of LC-ESI-MS method for sensitive, accurate and rapid determination of UC-781 in New Zealand white rabbit plasma. Talanta. 2011 Sep 30;85(4):2074-9. doi: 10.1016/j.talanta.2011.07.037. PubMed PMID: 21872060.

[3] Goddeeris C, Willems T, Houthoofd K, Martens JA, Van den Mooter G. Dissolution enhancement of the anti-HIV drug UC 781 by formulation in a ternary solid dispersion with TPGS 1000 and Eudragit E100. Eur J Pharm Biopharm. 2008 Nov;70(3):861-8. doi: 10.1016/j.ejpb.2008.07.006. PubMed PMID: 18691650.

[4] Goddeeris C, Willems T, Van den Mooter G. Formulation of fast disintegrating tablets of ternary solid dispersions consisting of TPGS 1000 and HPMC 2910 or PVPVA 64 to improve the dissolution of the anti-HIV drug UC 781. Eur J Pharm Sci. 2008 Aug 7;34(4-5):293-302. doi: 10.1016/j.ejps.2008.05.005. PubMed PMID: 18602800.

[5] Goddeeris C, Van den Mooter G. Free flowing solid dispersions of the anti-HIV drug UC 781 with Poloxamer 407 and a maximum amount of TPGS 1000: investigating the relationship between physicochemical characteristics and dissolution behaviour. Eur J Pharm Sci. 2008 Sep 2;35(1-2):104-13. doi: 10.1016/j.ejps.2008.06.010. PubMed PMID: 18644442.

6: Fletcher P, Kiselyeva Y, Wallace G, Romano J, Griffin G, Margolis L, Shattock R. The nonnucleoside reverse transcriptase inhibitor UC-781 inhibits human immunodeficiency virus type 1 infection of human cervical tissue and dissemination by migratory cells. J Virol. 2005 Sep;79(17):11179-86. PubMed PMID: 16103169; PubMed Central PMCID: PMC1193640.7: Van Herrewege Y, Michiels J, Van Roey J, Fransen K, Kestens L, Balzarini J, Lewi P, Vanham G, Janssen P. In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus microbicides. Antimicrob Agents Chemother. 2004 Jan;48(1):337-9. PubMed PMID: 14693562; PubMed Central PMCID: PMC310190.8: Damian F, Blaton N, Kinget R, Van den Mooter G. Physical stability of solid dispersions of the antiviral agent UC-781 with PEG 6000, Gelucire 44/14 and PVP K30. Int J Pharm. 2002 Sep 5;244(1-2):87-98. PubMed PMID: 12204568.9: Deferme S, Van Gelder J, Ingels F, Van den Mooter G, De Buck S, Balzarini J, Naesens L, De Clercq E, Kinget R, Augustijns P. Intestinal absorption characteristics of the low solubility thiocarboxanilide UC-781. Int J Pharm. 2002 Mar 2;234(1-2):113-9. PubMed PMID: 11839442.10: Damian F, Blaton N, Desseyn H, Clou K, Augustijns P, Naesens L, Balzarini J, Kinget R, Van den Mooter G. Solid state properties of pure UC-781 and solid dispersions with polyvinylpyrrolidone (PVP K30). J Pharm Pharmacol. 2001 Aug;53(8):1109-16. PubMed PMID: 11518020.1

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