ARC 239 dihydrochloride
- Product Name
- ARC 239 dihydrochloride
- CAS No.
- 55974-42-0
- Chemical Name
- ARC 239 dihydrochloride
- Synonyms
- ARC 239 (hydrochloride);ARC 239 dihydrochloride, 10 mM in DMSO;ARC 239 dihydrochloride, alpha2B adrenoceptor antagonist;2-(2-(4-(2-Methoxyphenyl)piperazin-1-yl)ethyl)-4,4-dimethylisoquinoline-1,3(2H,4H)-dione dihydrochloride;Adrenergic Receptor,adrenoceptor antagonist,inhibit,ARC 239,Beta Receptor,ARC239,BHT-920,ARC 239 dihydrochloride,UK 14,304,ARC-239,pig nasal mucosa,Inhibitor,phenylephrine
- CBNumber
- CB34718588
- Molecular Formula
- C24H30ClN3O3
- Formula Weight
- 443.97
- MOL File
- 55974-42-0.mol
ARC 239 dihydrochloride Property
- storage temp.
- Store at RT
- solubility
- <48.04mg/ml in H2O
- form
- solid
- color
- White
- Water Solubility
- Soluble to 100 mM in water
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H400Very toxic to aquatic life
H410Very toxic to aquatic life with long lasting effects
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P273Avoid release to the environment.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P330Rinse mouth.
P391Collect spillage. Hazardous to the aquatic environment
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- A766573
- Product name
- ARC239Dihydrochloride
- Packaging
- 2.5mg
- Price
- $180
- Updated
- 2021/12/16
- Product number
- B6508
- Product name
- ARC239dihydrochloride
- Packaging
- 25mg
- Price
- $471
- Updated
- 2021/12/16
- Product number
- API0009832
- Product name
- ARC-239 DIHYDROCHLORIDE
- Purity
- 95.00%
- Packaging
- 5G
- Price
- $2656.5
- Updated
- 2021/12/16
- Product number
- B6508
- Product name
- ARC239dihydrochloride
- Packaging
- 5mg
- Price
- $125
- Updated
- 2021/12/16
ARC 239 dihydrochloride Chemical Properties,Usage,Production
Uses
ARC 239 Dihydrochloride is a norepinephrine-serotonin reuptake inhibitor that can be used for treatment of vasomotor symptoms. ARC 239 Dihydrochloride is also an α2-adrenoceptor antagonist.
Biological Activity
arc 239 dihydrochloride is a selective antagonist of α2b adrenoceptor with pkd value of 8.8 [1].α2b adrenoceptor is a g-protein coupled receptor. α2-adrenergic receptors include three subtypes: α2a, α2b and α2c, which play an important role in regulating neurotransmitter release from adrenergic neurons in the central nervous system and from sympathetic nerves.arc 239 dihydrochloride is a selective α2b adrenoceptor antagonist. in rat brain, arc 239 inhibited the binding of 5-htia receptor radioligands 8-oh-dpat and rx 821002 to cortical membranes with ki values of 63.1 and 136 nm respectively, which suggested that arc 239 recognized 5-ht1a receptor [2]. treatment human platelets with arc 239 significantly inhibited platelet aggregation induced by adenosine diphosphate (adp), epinephrine and arachidonic acid and increased collagen/epinephrine closure time, which suggested that α2b adrenoceptor play a critical role in platelet aggregation [3]. in cervical samples isolated from pregnant rats, arc 239 effectively inhibited noradrenaline-stimulated contractions [4].in c57bl/6 mice with gastric mucosal damage induced by acidified ethanol, arc 239 (10.4 nm) antagonized gastroprotective effect induced by α2-adrenoceptor agonists [5].
IC 50
Alpha-2B adrenergic receptor; 5-HT1A Receptor
storage
Store at RT
References
[1]. bylund db, ray-prenger c, murphy tj. alpha-2a and alpha-2b adrenergic receptor subtypes: antagonist binding in tissues and cell lines containing only one subtype. j pharmacol exp ther, 1988, 245(2): 600-607.
[2]. meana jj, callado lf, pazos a, et al. the subtype-selective alpha 2-adrenoceptor antagonists brl 44408 and arc 239 also recognize 5-ht1a receptors in the rat brain. eur j pharmacol, 1996, 312(3): 385-388.
[3]. marketou me, kintsurashvili e, androulakis ne, et al. blockade of platelet alpha2b-adrenergic receptors: a novel antiaggregant mechanism. int j cardiol, 2013, 168(3): 2561-2566.
[4]. gál a, kolarovszki-sipiczki z, et al. the effect of the arc 239 on the myometrial and cervical action in the rat, in vitro. acta pharm hung, 2009, 79(2): 75-80.
[5]. zádori zs, shujaa n, brancati sb, et al. both α2b- and α2c-adrenoceptor subtypes are involved in the mediation of centrally induced gastroprotection in mice. eur j pharmacol, 2011, 669(1-3): 115-120.
ARC 239 dihydrochloride Preparation Products And Raw materials
Raw materials
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