Cl-Amidine
- Product Name
- Cl-Amidine
- CAS No.
- 1043444-18-3
- Chemical Name
- Cl-Amidine
- Synonyms
- Cl-amidine TFA;Cl-Amidine (trifluoroacetate salt);(2S)-5-(2-Chloroethanimidamido)-2-(phenylformamido)pentanamide trifluoroacetic acid salt
- CBNumber
- CB13053598
- Molecular Formula
- C14H19ClN4O2 ? CF3CO2H
- Formula Weight
- 424.81
- MOL File
- 1043444-18-3.mol
Cl-Amidine Property
- storage temp.
- under inert gas (nitrogen or Argon) at 2–8 °C
- solubility
- ≤20mg/ml in ethanol;50mg/ml in DMSO;14mg/ml in dimethyl formamide
- form
- crystalline solid
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
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
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
- 10599
- Product name
- Cl-Amidine (trifluoroacetate salt)
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $140
- Updated
- 2021/12/16
- Product number
- 10599
- Product name
- Cl-Amidine (trifluoroacetate salt)
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $35
- Updated
- 2021/12/16
- Product number
- 10599
- Product name
- Cl-Amidine (trifluoroacetate salt)
- Purity
- ≥95%
- Packaging
- 10mg
- Price
- $193
- Updated
- 2021/12/16
- Product number
- C3829
- Product name
- Cl-Amidine(trifluoroacetatesalt)
- Packaging
- 10mg
- Price
- $221
- Updated
- 2021/12/16
- Product number
- C3829
- Product name
- Cl-Amidine(trifluoroacetatesalt)
- Packaging
- 5mg
- Price
- $139
- Updated
- 2021/12/16
Cl-Amidine Chemical Properties,Usage,Production
Biological Activity
cl-amidine is a pad4 deimination activity inhibitor.protein arginine deiminase 4 (pad4) can catalyze the post-translational modification of arginine residues on histones to form citrulline, which can change gene expression. thus, dysregulated pad4 activity has been implicated in cancer and rheumatoid arthritis.
in vitro
previous study found that cl-amidine antagonized the pad4-mediated enhancement of the the p300gbd-grip1 interaction dose-dependently, and it was noteworthy that cl-amidine treatment had only a minimal reduction in the efficiency of the interaction in cys645s-transfected cells, thereby suggesting that the inhibitory effect of cl-amidine was not a nonspecific one but was targeted at the active pad4 enzyme. these results demonstrated that cl-amidine was significantly more potent than f-amidine, consistent with its improved in vitro potency [1].
in vivo
animal study showed that cl-amidine could improve survival in a mouse model of cecal ligation and puncture (clp)-induced septic shock. cl-amidine was proven to play protective roles by restoring innate immune cells in bm, decreasing bm and thymus atrophy, increasing blood monocytes and blood/liver bacteria clearance, and attenuating pro-inflammatory cytokine production in a murine lethal sepsis model [2].
target
| Target | Value |
| PAD1 (Cell-free assay) | 0.8 μM |
| PAD4 (Cell-free assay) | 5.9 μM |
| 6.2 μM |
IC 50
5.9 μm
References
[1] luo, y. ,arita, k.,bhatia, m., et al. inhibitors and inactivators of protein arginine deiminase 4: functional and structural characterization. biochemistry 45(39), 11727-11736 (2006).
[2] zhao t, pan b, alam hb, liu b, bronson rt, deng q, wu e, li y. protective effect of cl-amidine against clp-induced lethal septic shock in mice. sci rep. 2016 nov 7;6:36696.
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