WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 527073
CAS#: 928621-15-2 (HCl)
Description: L594881, also known as 3',4'-Dichlorobenzamil or DCB, is an inhibitor of Na+/Ca2+ exchanger, Na+ transport and sarcoplasmic reticulum Ca2+ release channels. L594881 can inhibit Na+/Ca2+ exchanger, Na+ transport and sarcoplasmic reticulum Ca2+ release channels.
MedKoo Cat#: 527073
Name: L594881 HCl
CAS#: 928621-15-2 (HCl)
Chemical Formula: C13H13Cl4N7O
Exact Mass: 422.9936
Molecular Weight: 425.095
Elemental Analysis: C, 36.73; H, 3.08; Cl, 33.36; N, 23.07; O, 3.76
Related CAS #: 928621-15-2 (HCl) 1166-01-4 (free base)
Synonym: 3',4'-Dichlorobenzamil HCl; Dichlorobenzamil; L594881; L-594881; L 594881; DCB.
IUPAC/Chemical Name: [Amino-[(3,5-diamino-6-chloropyrazine-2-carbonyl)amino]methylidene]-[(3,4-dichlorophenyl)methyl]azanium chloride
InChi Key: LPHAOBPPRPXQLQ-UHFFFAOYSA-N
InChi Code: InChI=1S/C13H12Cl3N7O.ClH/c14-6-2-1-5(3-7(6)15)4-20-13(19)23-12(24)8-10(17)22-11(18)9(16)21-8;/h1-3H,4H2,(H4,17,18,22)(H3,19,20,23,24);1H
SMILES Code: ClC1=CC=C(C/[NH+]=C(N)/NC(C2=NC(Cl)=C(N)N=C2N)=O)C=C1Cl.[Cl-]
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
| Biological target: | L594881, also known as 3',4'-Dichlorobenzamil or DCB, is an inhibitor of Na+/Ca2+ exchanger, Na+ transport and sarcoplasmic reticulum Ca2+ release channels. |
| In vitro activity: | Remarkably 3',4'-dichlorobenzamil hydrochloride a sodium-calcium exchange inhibitor, completely abolished excystation of Acanthamoeba. Reference: Parasit Vectors. 2019 Nov 14;12(1):538. https://pubmed.ncbi.nlm.nih.gov/31727139/ |
| In vivo activity: | This study found that the NCX inhibitor 3',4'-Dichlorobenzamil (DCB) can significantly inhibit the relaxation of rat bladder detrusor strips and a reduction of the [Ca(2+)]i induced by LCA, while the antagonist of muscarinic receptor and the agonist of the G protein-coupled bile acid receptor (TGR5) and the farnesoid X receptor (FXR) had no effect. Reference: Sci Rep. 2016 Feb 19;6:21358. https://pubmed.ncbi.nlm.nih.gov/26892434/ |
The following data is based on the product molecular weight 425.095 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Siddiqui R, Roberts SK, Ong TYY, Mungroo MR, Anwar A, Khan NA. Novel insights into the potential role of ion transport in sensory perception in Acanthamoeba. Parasit Vectors. 2019 Nov 14;12(1):538. doi: 10.1186/s13071-019-3785-0. PMID: 31727139; PMCID: PMC6857129. 2. Doleschal B, Primessnig U, Wölkart G, Wolf S, Schernthaner M, Lichtenegger M, Glasnov TN, Kappe CO, Mayer B, Antoons G, Heinzel F, Poteser M, Groschner K. TRPC3 contributes to regulation of cardiac contractility and arrhythmogenesis by dynamic interaction with NCX1. Cardiovasc Res. 2015 Apr 1;106(1):163-73. doi: 10.1093/cvr/cvv022. Epub 2015 Jan 28. PMID: 25631581; PMCID: PMC4362401. 3. Zhu J, Dong X, Liu Q, Wu C, Wang Q, Long Z, Li L. Hydrophobic bile acids relax rat detrusor contraction via inhibiting the opening of the Na⁺/Ca²⁺ exchanger. Sci Rep. 2016 Feb 19;6:21358. doi: 10.1038/srep21358. PMID: 26892434; PMCID: PMC4759538. 4. Kim JE, Choi BK, Choi JY, Ryu T, Roh WS, Song SY. Role of calcium channels responsible for phenylephrine-induced contraction in rat aorta 3 days after acute myocardial infarction. Korean J Anesthesiol. 2014 Feb;66(2):143-52. doi: 10.4097/kjae.2014.66.2.143. Epub 2014 Feb 28. PMID: 24624273; PMCID: PMC3948442. |
| In vitro protocol: | 1. Siddiqui R, Roberts SK, Ong TYY, Mungroo MR, Anwar A, Khan NA. Novel insights into the potential role of ion transport in sensory perception in Acanthamoeba. Parasit Vectors. 2019 Nov 14;12(1):538. doi: 10.1186/s13071-019-3785-0. PMID: 31727139; PMCID: PMC6857129. 2. Doleschal B, Primessnig U, Wölkart G, Wolf S, Schernthaner M, Lichtenegger M, Glasnov TN, Kappe CO, Mayer B, Antoons G, Heinzel F, Poteser M, Groschner K. TRPC3 contributes to regulation of cardiac contractility and arrhythmogenesis by dynamic interaction with NCX1. Cardiovasc Res. 2015 Apr 1;106(1):163-73. doi: 10.1093/cvr/cvv022. Epub 2015 Jan 28. PMID: 25631581; PMCID: PMC4362401. |
| In vivo protocol: | 1. Zhu J, Dong X, Liu Q, Wu C, Wang Q, Long Z, Li L. Hydrophobic bile acids relax rat detrusor contraction via inhibiting the opening of the Na⁺/Ca²⁺ exchanger. Sci Rep. 2016 Feb 19;6:21358. doi: 10.1038/srep21358. PMID: 26892434; PMCID: PMC4759538. 2. Kim JE, Choi BK, Choi JY, Ryu T, Roh WS, Song SY. Role of calcium channels responsible for phenylephrine-induced contraction in rat aorta 3 days after acute myocardial infarction. Korean J Anesthesiol. 2014 Feb;66(2):143-52. doi: 10.4097/kjae.2014.66.2.143. Epub 2014 Feb 28. PMID: 24624273; PMCID: PMC3948442. |
1: Sekizawa S, Bonham AC. Group I metabotropic glutamate receptors on second-order baroreceptor neurons are tonically activated and induce a Na+-Ca2+ exchange current. J Neurophysiol. 2006 Feb;95(2):882-92. Epub 2005 Sep 28. PubMed PMID: 16192328.
2: Lee K, Boden PR. Characterization of the inward current induced by metabotropic glutamate receptor stimulation in rat ventromedial hypothalamic neurones. J Physiol. 1997 Nov 1;504 ( Pt 3):649-63. PubMed PMID: 9401972; PubMed Central PMCID: PMC1159968.
