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| ln Vitro |
Cl-amidine hydrochloride is a haloacetamidine-based bioavailable drug that efficiently inhibits all active PAD isoenzymes (kinact/KI=13,000 M-1 min-1 for PAD4) [1 Cl-amidine hydrochloride (0, 5, 10, 15, 20, 25, 50 μg/mL, 24 hours) induces HT29 and TK6 lymphoblastoid cells. It displays the dose diagram on the round cell mold. compared to cells generated by Cl-amidine hydrochloride, the duct amidine series (HT29) is comparatively resistant [2]. In animal models, clonidine hydrochloride improves and inhibits neutrophil extracellular tray creation and histone 3 acidification [4].
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| ln Vivo |
Cl-amidine (75 mg/kg, intraperitoneal injection once daily) prevents and cures mice's DSS-induced cystitis [2]. Histological scores significantly decreased in response to clonidine (5, 25, 75 mg/kg, once daily via side wall gavage) in a dose-dependent manner [2].
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| Cell Assay |
Apoptosis analysis[2].
Cell Types: TK6 lymphoblastoid cells and HT29 colon cancer cells. Tested Concentrations: 0, 5, 10, 15, 20, 25, 50 μg/mL. Incubation Duration: 24 hrs (hours). Experimental Results: The induction of apoptosis was dose-dependent. |
| Animal Protocol |
Animal/Disease Models: C57BL/6 mice (8-12 weeks old, DSS colitis mouse model) [2].
Doses: 75 mg/kg. Management: IP one time/day. Experimental Results: Inhibition of PAD activity in vivo, protein citrullination, and PAD levels in the colon. Animal/Disease Models: C57BL/6 mice (8-12 weeks old, DSS colitis mouse model) [2]. Doses: 5, 25, 75 mg/kg. Route of Administration: po (oral gavage), one time/day. Experimental Results: Resultant in Dramatically lower histological scores. |
| 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.
[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. [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. [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. |
| Molecular Formula |
C14H20CL2N4O2
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|---|---|
| Molecular Weight |
347.24
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| CAS # |
1373232-26-8
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| Related CAS # |
D-Cl-amidine hydrochloride;Cl-amidine;913723-61-2;Cl-amidine TFA;1043444-18-3;D-Cl-amidine;1404060-15-6
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| SMILES |
O=C(N[C@H](C(N)=O)CCCNC(CCl)=N)C1=CC=CC=C1.[H]Cl
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| Chemical Name |
N-[(1S)-1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-benzamide Hydrochloride
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| Synonyms |
Cl amidine hydrochlorideCl amidine HClCl-amidine HCl Cl-amidine hydrochloride
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~143.99 mM)
H2O : ~50 mg/mL (~143.99 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.60 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (3.60 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (3.60 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5.5 mg/mL (15.84 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8799 mL | 14.3993 mL | 28.7985 mL | |
| 5 mM | 0.5760 mL | 2.8799 mL | 5.7597 mL | |
| 10 mM | 0.2880 mL | 1.4399 mL | 2.8799 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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