Alternate Text DC Chemicals' products qualify for U.S. tariff exemptions. We guarantee no price increases due to customs duties and maintain stable supply, continuing to deliver reliable research solutions to our American clients.
Home > Products > Novel inhibitors

ACT-451840

  Cat. No.:  DC46818   Featured
Chemical Structure
1984890-99-4
For research use only. We do not sell to patients.
We match the best price and quality on market.
Email:order@dcchemicals.com  sales@dcchemicals.com
Tel:+86-021-58447131
Get Quotation Now
We are official vendor of:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
More than 5000 active chemicals with high quality for research!
Field of application
ACT-451840 is an orally active, potent and low-toxicity compound, showing activity against sensitive and resistant plasmodium falciparum strains. ACT-451840 targets all asexual blood stages of the parasite, has a rapid onset of action. ACT-451840 behaves in a way similar to artemisinin derivatives, with very rapid onset of action and elimination of parasite. ACT-451840 can be used for the research of malarial.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1984890-99-4
Chemical Name: ACT-451840
Synonyms: SB18671;N-[[4-(4-acetylpiperazin-1-yl)phenyl]methyl]-3-(4-tert-butylphenyl)-N-[1-[4-[(4-cyanophenyl)methyl]p;ACT-451840
SMILES: O=C(C(CC1C=CC=CC=1)N(C(C=CC1C=CC(=CC=1)C(C)(C)C)=O)CC1C=CC(=CC=1)N1CCN(C(C)=O)CC1)N1CCN(CC2C=CC(C#N)=CC=2)CC1
Formula: C47H54N6O3
M.Wt: 750.970071315765
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. Bruderer S, et al. First-in-humans study of the safety, tolerability, and pharmacokinetics of ACT-451840, a new chemical entity with antimalarial activity. Antimicrob Agents Chemother. 2015;59(2):935-942. [2]. Boss C, et al. Discovery and Characterization of ACT-451840: an Antimalarial Drug with a Novel Mechanism of Action. ChemMedChem. 2016;11(18):1995-2014. [3]. Le Bihan A, et al. Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose-Efficacy Modeling. PLoS Med. 2016;13(10):e1002138. Published 2016 Oct 4.
Description: Use of ACT-451840 ACT-451840 is an orally active, potent and low-toxicity compound, showing activity against sensitive and resistant plasmodium falciparum strains. ACT-451840 targets all asexual blood stages of the parasite, has a rapid onset of action. ACT-451840 behaves in a way similar to artemisinin derivatives, with very rapid onset of action and elimination of parasite. ACT-451840 can be used for the research of malarial[1][2][3].
In Vivo: ACT-451840 (10 and 60 mg kg) starts to show significant antimalarial effects (parasite reduction) in vivo at 20 mg/kg. ACT-451840 exhibits curative activity at 300 mg/kg and significant antimalarial effects already at 100 mg/kg. ACT-451840 shows excellent reduction at 30 mg/kg, resulting in 99.80 % activity[2]. ACT-451840 shows efficacy in the Plasmodium berghei mouse model[2].
In Vitro: ACT-451840 shows a 50 % inhibition concentration of 0.4 nM against the drug-sensitive P. falciparum NF54 strain. The IC50 value of ACT-451840 against the murine malaria parasite P. berghei is 13.5 nM in in vitro ex vivo assays.
References: [1]. Bruderer S, et al. First-in-humans study of the safety, tolerability, and pharmacokinetics of ACT-451840, a new chemical entity with antimalarial activity. Antimicrob Agents Chemother. 2015;59(2):935-942. [2]. Boss C, et al. Discovery and Characterization of ACT-451840: an Antimalarial Drug with a Novel Mechanism of Action. ChemMedChem. 2016;11(18):1995-2014. [3]. Le Bihan A, et al. Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose-Efficacy Modeling. PLoS Med. 2016;13(10):e1002138. Published 2016 Oct 4.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC72999 CK-2-63 CK-2-63 is a potent first-in-class M. tuberculosis cytochrome bd (cyt bd) inhibitor, demonstrates growth suppression of M. tuberculosis H37Rv with IC50 of 3.7 uM.
DC72295 SpdSyn binder-1 SpdSyn binder-1 is a weak binder, which binds in the active site of plasmodium falciparum spermidine synthase. SpdSyn binder-1 can be used for the research of malaria.
DC70609 MMV030084 MMV030084 (MMV-030084) is a potent, specific P. falciparum cGMP-dependent protein kinase (PKG) inhibitor (Kdapp=9-16 nM), inhibits invasion of P. berghei ANKA parasites into HepG2 liver cells with IC50 of 199 nM.MMV030084 potently inhibits hepatocyte invasion by Plasmodium sporozoites, merozoite egress from asexual blood stage schizonts, and male gamete exflagellation, shows potent activity against liver, asexual, and sexual blood stage development.MMV030084 showed an IC50 of 109 nM against the drug-sensitive 3D7-A10 line, and an IC50 of 120 nM against multidrug-resistant Dd2-B2 parasites in a 72-h growth inhibition assay against Pf ABS parasites.MMV030084 inhibited male gamete exflagellation at an IC50 of 141 nM when gametocytes were stimulated to develop into male gametes.MMV030084 is a promising Plasmodium PKG-targeting chemotype.
DC70101 INE963 INE963 (INE-963) is a potent and fast-acting blood-stage antimalarial, demonstrates potent cellular activity against Pf 3D7 with EC50 of 6 nM in Pf growth inhibition assay.
DC70091 GSK3186899 GSK 3186899 (GSK-3186899, DDD853651) is a novel specific inhibitor of parasite cdc-2-related kinase 12 (CRK12), shows activity against L. donovani in intra-macrophage assay with EC50 value of 1.4 uM, and shows good selectivity against mammalian THP-1 host cells (EC50> 50 uM).
DC48830 GSK3494245 GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits (IC50=0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC50: purified 26S=13 µM; enriched THP-1 extracts IC50=40µM). GSK3494245 exhibits attractive biological and biosafety properties.
DC47399 MMV674850 MMV674850 is potent against asexual stage parasites at 2.7 and 4.5 nM and preferentially targets early-stage gametocytes (early-stage gametocyte: IC50 4.5 ± 3.6 nM; late-stage gametocyte: IC50 28.7 ± 0.2 nM).
DC47398 MMV666810 MMV666810, a 2-aminopyrazine similar to MMV390048, is potent against asexual parasites at 5.94 nM, but against gametocytes, it has a 3.3-fold selectivity to late-stage gametocytes compared to earlier stages (early-stage gametocyte: IC50 603 ± 88 nM; late-stage gametocyte: IC50 179 ± 8 nM).
DC46818 ACT-451840 ACT-451840 is an orally active, potent and low-toxicity compound, showing activity against sensitive and resistant plasmodium falciparum strains. ACT-451840 targets all asexual blood stages of the parasite, has a rapid onset of action. ACT-451840 behaves in a way similar to artemisinin derivatives, with very rapid onset of action and elimination of parasite. ACT-451840 can be used for the research of malarial.
DC43995 Conoidin A Conoidin A is a cell permeable inhibitor of T. gondii enzyme peroxiredoxin II (TgPrxII). Conoidin A covalently binds to the peroxidatic Cys47 of TgPrxII, irreversibly inhibiting its hyperperoxidation activity with an IC50 of 23 µM. Conoidin A also inhibit
X
Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
Site Map|Privacy PolicyCopyright © 2018-2020 All Rights Reserved. Technical Support:KuuJia