Cl-amidine hydrochloride |CAS 1373232-26-8|DC Chemicals

Cas No.:	1373232-26-8
SMILES:	O=C(N[C@H](C(N)=O)CCCNC(CCl)=N)C1=CC=CC=C1.[H]Cl
Formula:	C₁₄H₂₀Cl₂N₄O₂
M.Wt:	347.24
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

In Vitro Cl-amidine is a peptidylarginine deminase (PAD) inhibitor, with an IC50 of 5.9±0.3 μM for PAD4 and Cl-amidine is a bioavailable haloacetamidine-based compound that inhibits all the active PAD isozymes with near equal potency (kinact/KI=13,000 M-1.min-1 for PAD4). Cl-amidine induces apoptosis (identified as annexin V-positive/propidium iodide-negative cells) in such cells in a dose-dependent manner, indicating that Cl-amidine induces apoptosis of WBCs in vitro. Interestingly, the colon cancer cell line (HT29) is relatively resistant to apoptosis caused by Cl-amidine. In Vivo Significantly higher levels of colon inflammation in the 2% DSS than the 2% DSS+Cl-amidine mice are showed. The mean histology scores are 24.2±1.7 (SE) and 13.9±1.6, respectively. Most of the damage in the DSS-only group is in the distal colon, and this damage is suppressed with DSS+Cl-amidine. For the DSS-treated group, the mean colon length is 7.2±0.2 cm. In contrast, the average colon length of the DSS+Cl-amidine group is 8.4±0.2 cm, which is comparable to the mean colon lengths obtained for the wateralone and water+Cl-amidine groups (8.4±0.3 and 7.9±0.2 cm, respectively). The total distance and average speed of mice over a 96-h period are also measured. The results of these analyses demonstrate that the total distance is 5,072±381 and 3,190±401 m for the water-treated and DSS+Cl-amidine mice, but only 800±163 m for the DSS-only group. Similarly, the average speed on the wheel over the 4-day period is 6.2±0.63 and 5.3±0.58 m/min for the water-treated and DSS+Cl-amidine groups, but only 1.8±0.51 m/min for the DSS group.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC31074	Isopropyl myristate	Isopropyl myristate is the ester of isopropyl alcohol and myristic acid.
DC75868	AZ14133346	AZ14133346 (compound 36) is a potent and selective inhibitor of EGFR Exon20 insertions, with the IC50 of 85 nM. AZ14133346 plays an important role in cancer research.
DC75865	TI17	TI17 represents a novel class of targeted anticancer agents that specifically disrupt DNA damage repair mechanisms in malignant cells.
DC75816	Nisoxetine	Nisoxetine acts as a highly selective and potent noradrenaline transporter (NET) antagonist, exhibiting a binding affinity (Kd) of 0.76 nM. In addition to its antidepressant properties, nisoxetine functions as a local anesthetic by inhibiting voltage-gated sodium channels. This dual pharmacological activity makes it a compound of interest for both neurological and pain management research.
DC75202	Fosaprepitant free acid	Fosaprepitant, also known as MK0517, is an antiemetic drug, administered intravenously. It is a prodrug of aprepitant. Fosaprepitant was developed by Merck & Co. and was approved. It is a prodrug of Aprepitant. It aids in the prevention of acute and delayed nausea and vomiting associated with chemotherapy treatment. Fosaprepitant is a weak inhibitor of CYP3A4, and aprepitant, the active moiety, is a substrate, inhibitor, and inducer of CYP3A4
DC74684	ZH8667	ZH8667 is a trace amine-associated receptor 1 (TAAR1)–Gs agonist.
DC74646	EB-PSMA-617	EB-PSMA-617 is an Evans blue-modified prostate-specific membrane antigen (PSMA) 617 ligand for making 177Lu-EB-PSMA, which is potential useful for Metastatic Castration-Resistant Prostate Cancer.
DC74641	HC-258	HC-258 is a Covalent Acrylamide TEAD Inhibitor That Reduces Gene Expression and Cell Migration. HC-258 reduces the CTGF, CYR61, AXL, and NF2 transcript levels and inhibits the migration of MDA-MB-231 breast cancer cells. Co-crystallization with hTEAD2 confirmed that HC-258 binds within TEAD’s PA pocket, where it forms a covalent bond with its cysteine.
DC74639	Oligopeptide-10	Oligopeptide-10, also known as granactive oligopeptide-10, is a synthetic bio-active peptide composed of 15 amino acids. it can help manage acne-causing bacteria, both on its own and in conjunction with anti-acne superstar exfoliant salicylic acid.
DC74638	GLPG3667	GLPG3667 is an oral, reversible, and selective tyrosine kinase 2 (TYK2) inhibitor. It is being developed to treat inflammatory and auto-immune diseases. Biochemical assays showed that GLPG3667 displayed nanomolar potency on TYK2 with a selectivity over other JAK kinases >3-fold. In human PBMC, GLPG3667 showed comparable potency on the IFNα and IL-23 pathways (around 50 nM). Selectivity for TYK2 on the IFNα pathway was >14-fold and >19-fold toward the IL-2 and GM-CSF pathways in human PBMC and whole blood, respectively. Dermal ear inflammation in a mouse model of psoriasis driven by IL-23 was prevented by GLPG3667 with a minimal effective dose of 3 mg/kg given orally once daily. This effect was associated with a decrease in neutrophil infiltration and STAT3 phosphorylation at sites of inflammation. In healthy HV, GLPG3667 completely inhibited IFNα-induced STAT1 and STAT3 phosphorylation but did not impact IL-2- and GM-CSF-induced STAT5 phosphorylation.