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
Cl-Amidine Property
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
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.
N-Bromosuccinimide Price
- 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
- 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
- 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
- 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
- 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
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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