Proguanil

产品编号: DC10397
Proguanil
结构式
500-92-5
此产品仅供科研所需,我们不出售给病人
​我们将匹配市场上最好的价格给您
Email:order@dcbio.cn
免费咨询电话:4008862077
我们的合作伙伴:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
中国地区超过5000个高品质化合物库存
应用领域
Proguanil is an antimalarial prodrug that is metabolized to the active metabolite cycloguanil, a dihydrofolate reductase (DHFR) inhibitor.
Cas No.: 500-92-5
名称:
别名:
SMILES: N=C(NC1=CC=C(Cl)C=C1)NC(NC(C)C)=N
分子式: C11H16ClN5
分子量: 253.73
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: Proguanil per se has only weak antimalarial activity in vitro (IC50=2.4-19 μM), and its effectiveness depends on the active metabolite cycloguanil (IC50=0.5-2.5 nM). The cycloguanil is a dihydrofolate reductase (DHFR) inhibitor. The combination of atovaquone and proguanil is synergistic in vitro. Both drugs also have activity against gametocytes and pre-erythrocytic (hepatic) stages of malaria parasites. Proguanil acts as a biguanide rather than as its metabolite cycloguanil (a parasite dihydrofolate reductase [DHFR] inhibitor) to enhance the atovaquone effect; proguanil-mediated enhancement is specific for atovaquone, since the effects of other mitochondrial electron transport inhibitors, such as myxothiazole and antimycin, are not altered by inclusion of proguanil. 5-HT3 receptor responses are reversibly inhibited by proguanil, the metabolite 4-chlorophenyl-1-biguanide (CPB) and the active metabolite cycloguanil (CG), with an IC50 of 1.81, 1.48 and 4.36 μM, respectively.Proguanil could induce infertility in rats which may act by distorting the blood-testis barrier formed by the Sertoli cells. Duration dependent significant decrease in body and organ weights and also in sperm parameters is observed. Serum testosterone level is significantly decreased for proguanil treatment rats. Administration of Malarone (atovaquone and proguanil) to experimentally B. gibsoni infected two dogs in chronic stage and three dogs in acute stage results in decrease in parasitemia, and clinical improvements are observed[5].
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
产品编号 产品名称 应用领域
DC9692 Volitinib(Savolitinib) Savolitinib(Volitinib; AZD-6094; Volitinib) is an orally bioavailable inhibitor of the c-Met receptor tyrosine kinase(IC50= 5 nM) with potential antineoplastic activity.
DC9574 A-317491 (sodium salt hydrate) A-317491 is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors.
DC9545 Miglustat (hydrochloride) Miglustat hydrochloride is an inhibitor of glucosylceramide synthase, primarily to treat Type I Gaucher disease (GD1).
DC9542 MPTP (hydrochloride) MPTP HCl induced reduction in the DOPAC HVA/dopamine (DA) ratio and increase in striatal ascorbate (AS) oxidation in rats
DC9536 Sertindole Sertindole, a neuroleptic, is one of the newer antipsychotic medications available.
DC9505 Pifithrin-α (hydrobromide) Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes.
DC9459 SB 415286 SB 415286 is a potent and selective cell-permeable, ATP-competitive inhibitor of GSK3α with an IC50 value of 78 nM (similar potency for GSK3β) and a Ki value of 31 nM.
DC9442 PF-04457845 PF-04457845 is a potent and exquisitely selective inhibitor of FAAH, with an IC50 of 7.2 nM, and both analgesic and antiinflammatory effects in animal studies comparable to naproxen.
DC9402 Letermovir AIC246 is a novel anti-CMV compound which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.
DC9388 RS 504393 RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 98 nM and > 100 μM for inhibition of human recombinant CCR2b and CCR1 receptors respectively).