Cl-Amidine

Product Name: Cl-Amidine
CAS No.: 913723-61-2
Chemical Name: Cl-Amidine
Synonyms: Cl-Amidine;N-BCl-I-OA cpd;Cl amidine,Clamidine;N-alpha-Benzoyl-N5-(2-chloro-1-iminoethyl)-1-ornithine amide;(S)-N-(1-Amino-5-(2-chloroacetimidamido)-1-oxopentan-2-yl)benzamide;N-[(1S)-1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]benzamide;Benzamide, N-[(1S)-1-(aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-;N-[(1S)-1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-benzamideN-
CBNumber: CB62590660
Molecular Formula: C14H19ClN4O2
Formula Weight: 310.78
MOL File: 913723-61-2.mol

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Cl-Amidine Property

storage temp.: Store at -20°C
solubility: Soluble in DMSO

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

J&W Pharmlab

Product number: 15R0242
Product name: N-[(1S)-1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-benzamide
Purity: 94%
Packaging: 10mg
Price: $98
Updated: 2021/12/16

J&W Pharmlab

Product number: 15R0242
Product name: N-[(1S)-1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-benzamide
Purity: 94%
Packaging: 100mg
Price: $498
Updated: 2021/12/16

J&W Pharmlab

Product number: 15R0242
Product name: N-[(1S)-1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-benzamide
Purity: 94%
Packaging: 250mg
Price: $698
Updated: 2021/12/16

J&W Pharmlab

Product number: 15R0242
Product name: N-[(1S)-1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-benzamide
Purity: 94%
Packaging: 500mg
Price: $998
Updated: 2021/12/16

J&W Pharmlab

Product number: 15R0242
Product name: N-[(1S)-1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-benzamide
Purity: 94%
Packaging: 1g
Price: $1698
Updated: 2021/12/16

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Cl-Amidine Chemical Properties,Usage,Production

Uses

Cl-amidine is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine induces apoptosis in cancer cells. Cl-amidine induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model[1][2][3][4][5].

Definition

ChEBI: Cl-Amidine is a member of benzenes.

Biological Activity

Cl-amidine is an orally active PAD inhibitor with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3 and PAD4, respectively.It induces apoptosis in cancer cells. And Cl-Amidine blocks histone 3 citrullination and neutrophil extracellular trap formation and improves survival in mice with sepsis.

in vivo

Cl-amidine (75 mg/kg, ip once daily) suppresses and treats DSS-induced colitis in mice^[2].
Cl-amidine (5, 25, 75 mg/kg, oral gavage, once daily) leads to significant reductions in the histology scores dose-dependently^[2].

Animal Model:	C57BL/6 mice (8-12 wk old, DSS mouse model of colitis)^[2].
Dosage:	75 mg/kg.
Administration:	IP once daily.
Result:	Suppressed PAD activity, protein citrullination, and PAD levels in the colon in vivo.

Animal Model:	C57BL/6 mice (8-12 wk old, DSS mouse model of colitis)^[2].
Dosage:	5, 25, 75 mg/kg.
Administration:	Oral gavage once daily.
Result:	Led to significant reductions in the histology scores.

target

IC50: 0.8 μM (PAD1), 5.9 μM (PAD4), 6.2 μM (PAD3).

References

[1] Yuan Luo, et al. Inhibitors and Inactivators of Protein Arginine Deiminase 4: Functional and Structural Characterization. Biochemistry. 2006 Oct 3; 45(39): 11727–11736. DOI:10.1021/bi061180d
[2] Chumanevich AA, et al. Suppression of colitis in mice by Cl-amidine: a novel peptidylarginine deiminase inhibitor. Am J Physiol Gastrointest Liver Physiol. 2011 Jun;300(6):G929-38. DOI:10.1152/ajpgi.00435.2010
[3] Witalison EE, et al. Molecular targeting of protein arginine deiminases to suppress colitis and prevent colon cancer. Oncotarget. 2015 Nov 3;6(34):36053-62. DOI:10.18632/oncotarget.5937
[4] Biron BM, et al., Cl-Amidine Prevents Histone 3 Citrullination and Neutrophil Extracellular Trap Formation, and Improves Survival in a Murine Sepsis Model. J Innate Immun. 2017;9(1):22-32. DOI:10.1159/000448808
[5] Bryan Knuckley, et al. Substrate Specificity and Kinetic Studies of PADs 1, 3, and 4 Identify Potent and Selective Inhibitors of Protein Arginine Deiminase 3. Biochemistry. 2010 Jun 15;49(23):4852-63. DOI:10.1021/bi100363t

Cl-Amidine Preparation Products And Raw materials

Raw materials

Preparation Products

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Cl-Amidine Suppliers

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913723-61-2, Cl-AmidineRelated Search:

Cl-Amidine

N-[(1S)-1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-benzamideN-

N-[(1S)-1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]benzamide

N-alpha-Benzoyl-N5-(2-chloro-1-iminoethyl)-1-ornithine amide

Benzamide, N-[(1S)-1-(aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-

Cl amidine,Clamidine

N-BCl-I-OA cpd

(S)-N-(1-Amino-5-(2-chloroacetimidamido)-1-oxopentan-2-yl)benzamide

913723-61-2