Ganaplacide
Ganaplacide (KAF156) is a first-in-class, orally active imidazolopiperazine antimalarial agent. Ganaplacide is active against a broad range of Plasmodium species, including drug-resistant parasites. Ganaplacide is parasiticidal against both asexual and sexual blood stages as well as the liver stages of the parasite.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1261113-96-5
- 分子式: C22H23F2N5O
- 分子量:411.45
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
Parasite アイソフォーム固有の製品をすべて表示
More
生物活性
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | CC50 |
>12 μM
Compound: 22
|
Cytotoxicity against mouse BA/F3 cells
Cytotoxicity against mouse BA/F3 cells
|
[PMID: 22524250] |
| CHO | CC50 |
>12 μM
Compound: 22
|
Cytotoxicity against CHO cells
Cytotoxicity against CHO cells
|
[PMID: 22524250] |
| CHO | IC50 |
13.4 μM
Compound: 22
|
Inhibition of human ERG channel expressed in CHO cells by patch clamp assay
Inhibition of human ERG channel expressed in CHO cells by patch clamp assay
|
[PMID: 22524250] |
| HEK-293T | CC50 |
>12 μM
Compound: 22
|
Cytotoxicity against human 293T cells
Cytotoxicity against human 293T cells
|
[PMID: 22524250] |
| HeLa | CC50 |
>12 μM
Compound: 22
|
Cytotoxicity against human HeLa cells
Cytotoxicity against human HeLa cells
|
[PMID: 22524250] |
| HEp-2 | CC50 |
>12 μM
Compound: 22
|
Cytotoxicity against human Hep2 cells
Cytotoxicity against human Hep2 cells
|
[PMID: 22524250] |
| Huh-7 | CC50 |
>12 μM
Compound: 22
|
Cytotoxicity against human HuH7 cells
Cytotoxicity against human HuH7 cells
|
[PMID: 22524250] |
Ganaplacide (KAF156) shows blood schizonticidal activity with 50% inhibitory concentrations of 6 to 17.4 nM against P. falciparum drug-sensitive and drug-resistant strains[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ganaplacide (KAF156) (1-15 mg/kg; p.o.) is fully protective in a causal prophylactic mouse model of malaria[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Mice (causal prophylactic rodent malaria model)[1]
-
Dosage:1-15 mg/kg
-
Administration:p.o.
-
Result:A single oral dose of 10 mg of KAF156/kg administered 2 h before infection was fully protective.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 1261113-96-5
-
分子量 411.45
-
分子式 C22H23F2N5O
-
SMILES
FC(C=C1)=CC=C1C2=C(N3C(C(C)(N(C(CN)=O)CC3)C)=N2)NC4=CC=C(F)C=C4
-
別名
KAF156; GNF156
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Leong FJ, et al. A first-in-human randomized, double-blind, placebo-controlled, single- and multiple-ascending oral dose study of novel Imidazolopiperazine KAF156 to assess its safety, tolerability, and pharmacokinetics in healthy adult volunteers. Antimicrob Agents Chemother. 2014;58(11):6437-6443. [Content Brief]
[2]. Kuhen KL, et al. KAF156 is an antimalarial clinical candidate with potential for use in prophylaxis, treatment, and prevention of disease transmission. Antimicrob Agents Chemother. 2014;58(9):5060-5067. [Content Brief]
[3]. Leong FJ, et al. A first-in-human randomized, double-blind, placebo-controlled, single- and multiple-ascending oral dose study of novel Imidazolopiperazine KAF156 to assess its safety, tolerability, and pharmacokinetics in healthy adult volunteers. Antimicrob Agents Chemother. 2014;58(11):6437-6443. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Ganaplacide 関連分類
HY-108024 関連分類
Powered by Bioz