Alternate TextTo enhance service speed and avoid tariff delays, we've opened a US warehouse. All US orders ship directly from our US facility.
Home > Products > Novel inhibitors

Emedastine

  Cat. No.:  DC39705   Featured
Chemical Structure
87233-61-2
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
Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 87233-61-2
Chemical Name: Emedastine
SMILES: CN1CCCN(C2N(CCOCC)C3C(=CC=CC=3)N=2)CC1
Formula: C17H26N4O
M.Wt: 302.414
Purity: >98%
Sotrage: 2 years -20°C powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. Sharif NA, et al. Emedastine: a potent, high affinity histamine H1-receptor-selective antagonist for ocular use: receptor binding and second messenger studies. J Ocul Pharmacol. 1994 Winter;10(4):653-64. [2]. Murota H, et al. Emedastine difumarate: a review of its potential ameliorating effect for tissue remodeling in allergic diseases. Expert Opin Pharmacother. 2009 Aug;10(11):1859-67. [3]. Andoh T, et al. Involvement of blockade of leukotriene B(4) action in anti-pruritic effects of emedastine in mice. Eur J Pharmacol. 2000 Oct 6;406(1):149-52.
Description: Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis[1][2][3].
Target: H1 Receptor:1.3 nM (Ki) H2 Receptor:49067 nM (Ki) H3 Receptor:12430 nM (Ki)
In Vivo: Emedastine (0.03, 0.1, 0.3 mg/kg; orally; pretreatment of 30 min) significantly suppresses histamine-induced scratching with 0.1 and 0.3 mg/kg but not 0.03 mg/kg[3]. Pretreatment with Emedastine (0.03, 0.1, 0.3 mg/kg; orally) significantly inhibits the scratching induced by substance P and leukotriene B[3]. Emedastine (0.3 mg/kg, p.o.) produces significant inhibition of passive peritoneal anaphylaxis in guinea-pigs[2]. Emedastine inhibits histamine-induced contractions of isolated ileum (IC50=6.1 nM)[2]. Animal Model: Male ICR mice 5-6 weeks of age[3] Dosage: 0.03, 0.1, 0.3 mg/kg Administration: Orally; 30 min before pruritogen injection Result: Significantly suppressed histamine-induced scratching with pretreatment of 0.1 and 0.3 mg/kg.
In Vitro: Emedastine inhibits histamine H2 receptor (Ki=49067 nM) and histamine H3 receptor (Ki=12430 nM)[1]. High concentrations of Emedastine (1 and 10 ng/ml) significantly inhibits type 1 collagen production in normal human dermal fibroblasts[2]. Emedastine (1, 10, 100, 1000 nM) at concentrations of ≥ 10 nM inhibits CC chemokine-elicited eosinophil migration[2].
References: [1]. Sharif NA, et al. Emedastine: a potent, high affinity histamine H1-receptor-selective antagonist for ocular use: receptor binding and second messenger studies. J Ocul Pharmacol. 1994 Winter;10(4):653-64. [2]. Murota H, et al. Emedastine difumarate: a review of its potential ameliorating effect for tissue remodeling in allergic diseases. Expert Opin Pharmacother. 2009 Aug;10(11):1859-67. [3]. Andoh T, et al. Involvement of blockade of leukotriene B(4) action in anti-pruritic effects of emedastine in mice. Eur J Pharmacol. 2000 Oct 6;406(1):149-52.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC60859 MT-125(MT 125) MT125​​ is a brain-penetrant small-molecule inhibitor selectively targeting non-muscle myosin IIA/B (NMIIA/B) with >20-fold specificity over cardiac myosin. It demonstrates potent anti-glioblastoma activity by: (1) blocking tumor invasion and cytokinesis (inducing polyploidy), (2) disrupting mitochondrial dynamics to elevate ROS and trigger ferroptosis, and (3) sensitizing tumors to radiotherapy/kinase inhibitors via ROS-driven PDGFR/mTOR pathway activation. Subcutaneous administration achieves brain concentrations twice plasma levels (t1/2~10.5 hr) with no toxicity observed at 15× the therapeutic dose in rats. MT-125 monotherapy extends survival in GBM models, while combinations with PDGFR/PI3K inhibitors induce long-term remission (>40% mice). Its first-in-class mechanism, safety profile, and CNS bioavailability support clinical development for glioblastoma.
DC60781 TRPC6 activator compound 2 TRPC6 activator compound 2 is selective activator of TRPC6 that does not potentiate TRPC3 and mTRPC7. Comp2 is able to cross BBB.
DC66546 R-Sirpiglenastat R-Sirpiglenastat is the R- isomer of Sirpiglenastat(DRP-104).Sirpiglenastat (DRP104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response.
DC60597 AZD0780 AZD0780 is the first oral small molecule PCSK9 inhibitor for the treatment of hypercholesterolemia.
DC90056 PLX-5622 HCl form (water solubility form) PLX5622 is the HCl salt form of PLX-5622, which has better water solubility.PLX-5622 is a highly selective brain-penetrant CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM) allowing for extended and specific microglial elimination, preceding and during pathology development.
DC65830 1-M-PES(1-Methoxy-5-methylphenazinium ethyl sulfate) 1-m-PES is an electron mediator which has higher stability of solutions than 1-Methoxy PMS. The stability in neutral to alkali conditions has been extremely improved with 1-Methoxy PES. 1-M-PES is a stable small-molecular compound and it has an equal or higher thermal stability than diaphorase. The 1-Methoxy PES solution can be stored long term.
DC65821 Upadacitinib hemihydrate Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor with an IC50 of 43 nM, being developed for the treatment of several autoimmune disorders.
DC65697 HDAC6 inhibitor 4510 A novel and seletive HDAC6 inhibitor.
DC65676 Fenretinide Glucuronide Monosodium Salt Fenretinide Glucuronide Monosodium Salt, is the metabolite of Fenretinide (F250000), which is a synthetic retinoid deriverative, substances related to vitamin A. They are also shown to be used for the treatment of cancer, as well as in the treatment of cystic fibrosis, rheumatoid arthritis, acne, and psoriasis.
DC89083 Pacritinib citrate Pacritinib Citrate is the citrate salt form of pacritinib, an orally bioavailable inhibitor of Janus kinase 2 (JAK2).
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