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301297-45-0
  • names:

    1-(cyclopropylmethyl)-6-(3,5-dimethylbenzoyl)-5-isopropylpyrimidine-2,4(1H,3H)-dione

  • CAS号:

    301297-45-0

    MDL Number:
  • MF(分子式): C20H24N2O3 MW(分子量): 340.423
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
IQP-0528
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中文别名 IQP-0528
英文别名 IQP-0528; IQP 0528; IQP0528; SJ-3991; SJ3991; SJ3991
CAS号 301297-45-0
SMILES O=C1NC(C(C(C)C)=C(C(C2=CC(C)=CC(C)=C2)=O)N1CC3CC3)=O
Inchi InChI=1S/C20H24N2O3/c1-11(2)16-17(18(23)15-8-12(3)7-13(4)9-15)22(10-14-5-6-14)20(25)21-19(16)24/h7-9,11,14H,5-6,10H2,1-4H3,(H,21,24,25)
InchiKey UCOAKFIVSAVHLC-UHFFFAOYSA-N
分子式 Formula C20H24N2O3
分子量 Molecular Weight 340.423
闪点 FP
熔点 Melting point
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
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 IQP-0528(CAS:301297-45-0):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。
IntroductionIQP-0528, also known as SJ-3991, is a non-nucleoside reverse transcriptase inhibitor potentially for the treatment of HIV infection. IQP-0528 works by blocking virus entry and has shown antiviral activity as microbicide gels.
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]Pereira LE, Mesquita PM, Ham A, Singletary T, Deyounks F, Martin A, McNicholl J, Buckheit KW, Buckheit RW Jr, Smith JM. Pharmacokinetic and Pharmacodynamic Evaluation following Vaginal Application of IQB3002, a Dual-Chamber Microbicide Gel Containing the Nonnucleoside Reverse Transcriptase Inhibitor IQP-0528 in Rhesus Macaques. Antimicrob Agents Chemother. 2015 Dec 14;60(3):1393-400. doi: 10.1128/AAC.02201-15. PubMed PMID: 26666935; PubMed Central PMCID: PMC4775942.
[2]Srinivasan P, Zhang J, Martin A, Kelley K, McNicholl JM, Buckheit RW Jr, Smith JM, Ham AS. Safety and Pharmacokinetics of Quick-Dissolving Polymeric Vaginal Films Delivering the Antiretroviral IQP-0528 for Preexposure Prophylaxis. Antimicrob Agents Chemother. 2016 Jun 20;60(7):4140-50. doi: 10.1128/AAC.00082-16. PubMed PMID: 27139475; PubMed Central PMCID: PMC4914618.
[3] Dezzutti CS, Shetler C, Mahalingam A, Ugaonkar SR, Gwozdz G, Buckheit KW, Buckheit RW Jr. Safety and efficacy of tenofovir/IQP-0528 combination gels - a dual compartment microbicide for HIV-1 prevention. Antiviral Res. 2012 Nov;96(2):221-5. doi: 10.1016/j.antiviral.2012.08.004. PubMed PMID: 22940075; PubMed Central PMCID: PMC3501576.
[4] Ham AS, Rohan LC, Boczar A, Yang L, W Buckheit K, Buckheit RW Jr. Vaginal film drug delivery of the pyrimidinedione IQP-0528 for the prevention of HIV infection. Pharm Res. 2012 Jul;29(7):1897-907. doi: 10.1007/s11095-012-0715-7. PubMed PMID: 22392331; PubMed Central PMCID: PMC4405790.
[5] Ham AS, Ugaonkar SR, Shi L, Buckheit KW, Lakougna H, Nagaraja U, Gwozdz G, Goldman L, Kiser PF, Buckheit RW Jr. Development of a combination microbicide gel formulation containing IQP-0528 and tenofovir for the prevention of HIV infection. J Pharm Sci. 2012 Apr;101(4):1423-35. doi: 10.1002/jps.23026. PubMed PMID: 22227864.
6: Mahalingam A, Simmons AP, Ugaonkar SR, Watson KM, Dezzutti CS, Rohan LC, Buckheit RW Jr, Kiser PF. Vaginal microbicide gel for delivery of IQP-0528, a pyrimidinedione analog with a dual mechanism of action against HIV-1. Antimicrob Agents Chemother. 2011 Apr;55(4):1650-60. doi: 10.1128/AAC.01368-10. PubMed PMID: 21245437; PubMed Central PMCID: PMC3067148.7: Ugaonkar SR, Clark JT, English LB, Johnson TJ, Buckheit KW, Bahde RJ, Appella DH, Buckheit RW Jr, Kiser PF. An Intravaginal Ring for the Simultaneous Delivery of an HIV-1 Maturation Inhibitor and Reverse-Transcriptase Inhibitor for Prophylaxis of HIV Transmission. J Pharm Sci. 2015 Oct;104(10):3426-39. doi: 10.1002/jps.24551. PubMed PMID: 26149293; PubMed Central PMCID: PMC4822498.8: Ham AS, Nugent ST, Peters JJ, Katz DF, Shelter CM, Dezzutti CS, Boczar AD, Buckheit KW, Buckheit RW Jr. The rational design and development of a dual chamber vaginal/rectal microbicide gel formulation for HIV prevention. Antiviral Res. 2015 Aug;120:153-64. doi: 10.1016/j.antiviral.2015.06.010. PubMed PMID: 26093158; PubMed Central PMCID: PMC4492852.9: Rastogi R, Teller RS, Mesquita PM, Herold BC, Kiser PF. Osmotic pump tablets for delivery of antiretrovirals to the vaginal mucosa. Antiviral Res. 2013 Oct;100(1):255-8. doi: 10.1016/j.antiviral.2013.08.007. PubMed PMID: 23973812; PubMed Central PMCID: PMC3924427.10: Mesquita PM, Srinivasan P, Johnson TJ, Rastogi R, Evans-Strickfaden T, Kay MS, Buckheit KW, Buckheit RW Jr, Smith JM, Kiser PF, Herold BC. Novel preclinical models of topical PrEP pharmacodynamics provide rationale for combination of drugs with complementary properties. Retrovirology. 2013 Oct 24;10:113. doi: 10.1186/1742-4690-10-113. PubMed PMID: 24156604; PubMed Central PMCID: PMC3827994.1
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