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Sarpogrelate hydrochloride

Product Name
Sarpogrelate hydrochloride
CAS No.
135159-51-2
Chemical Name
Sarpogrelate hydrochloride
Synonyms
SARPOGRELATE HCL;Anplag;MCI 9042;LS187,118;LS 187,118;LS-187,118;Sarpogrelate-D3 HCl;Sarpogrelate hydroch;SARPOGRELATE HYDROCHLORIDE;Sarpogrelate Hydrochloride RS
CBNumber
CB6511456
Molecular Formula
C24H32ClNO6
Formula Weight
465.96698
MOL File
135159-51-2.mol
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Sarpogrelate hydrochloride Property

Melting point:
145-148°C
storage temp. 
Inert atmosphere,2-8°C
solubility 
deionized water: ≥5mg/mL
form 
solid
InChIKey
POQBIDFFYCYHOB-UHFFFAOYSA-N
CAS DataBase Reference
135159-51-2(CAS DataBase Reference)
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Safety

Hazard Codes 
Xn,N
Risk Statements 
22-50/53
Safety Statements 
60-61
RIDADR 
UN 3077 9 / PGIII
WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H400Very toxic to aquatic life

Precautionary statements

P273Avoid release to the environment.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
S5451
Product name
Sarpogrelate hydrochloride
Purity
≥98% (HPLC)
Packaging
5mg
Price
$84.7
Updated
2024/03/01
Sigma-Aldrich
Product number
S5451
Product name
Sarpogrelate hydrochloride
Purity
≥98% (HPLC)
Packaging
25mg
Price
$269
Updated
2024/03/01
Cayman Chemical
Product number
24194
Product name
Sarpogrelate (hydrochloride)
Purity
≥98%
Packaging
10mg
Price
$87
Updated
2024/03/01
Cayman Chemical
Product number
24194
Product name
Sarpogrelate (hydrochloride)
Purity
≥98%
Packaging
50mg
Price
$299
Updated
2024/03/01
Cayman Chemical
Product number
24194
Product name
Sarpogrelate (hydrochloride)
Purity
≥98%
Packaging
100mg
Price
$553
Updated
2024/03/01
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Sarpogrelate hydrochloride Chemical Properties,Usage,Production

Description

Sarpogrelate hydrochloride, a potent and selective serotonin 5-HT2 receptor antagonist, was launched in Japan as an antithrombotic. It exhibits inhibition of ex vivo platelet aggregation stimulated by serotonin in combination with collagen and suppression of blood vessel constriction mediated by 5-HT2 in vitro. Its antithrombotic effects have been demonstrated in several in vivo experimental models including reduction of the mortality rate in acute pulmonary thromboembolic disease, arterial thrombosis, and peripheral obstructive disease. Sarpogrelate has been shown to be especially useful as an antiplatelet agent for patients with Type 2 diabetes mellitus, in whom 5-HT2mediated amplification of collageninduced platelet aggregation is significantly increased.

Description

Sarpogrelate is a selective antagonist of the serotonin (5-HT) receptor subtypes 5-HT2A, 5-HT2B, and 5-HT2C (Kis = 3.02, 269, and 37.2 nM, respectively, for human recombinant receptors expressed in CHO-K1 cells). It is selective for 5-HT2 (Ki = 70.8 nM) over 5-HT1 (Ki = >26,000 nM), α1-, α2-, and β-adrenergic (Kis = 640-123,800 nM), and muscarinic receptors (Ki = >40,000 nM). In vitro, it inhibits aggregation of rat whole blood induced by collagen, 5-HT with collagen, and 5-HT with ADP (; IC50s = 57.7, 0.56, and 22.7 μM, respectively). In vivo, it inhibits leukocyte-endothelial interactions in the femoral artery induced by a high-fat high-fructose diet (HFFD) in mice when administered at a dose of 5 mg/kg per day. Sarpogrelate (5 mg/kg per day) decreases ventricular hypertrophy and infarct size in a rat model of myocardial infarction.

Chemical Properties

White Solid

Originator

Mitsubishi Kasei (Japan )

Uses

Sarpogrelate hydrochloride is a potent and selective 5-HT2A receptor antagonist ress-induced hemolysis.

Definition

ChEBI: Sarpogrelate hydrochloride is a stilbenoid.

brand name

Anplag

Biological Activity

Selective 5-HT 2A receptor antagonist (pK i values are 8.52, 7.43 and 6.57 for 5-HT 2A , 5-HT 2C and 5-HT 2B receptors respectively). Displays selectivity over 5-HT 1 , 5-HT 3 , 5-HT 4 H 1 , H 2 , M 3 , α 1 -adrenergic, α 2 -adrenergic and β -adrenergic receptors. Displays cardioprotective activity in vivo .

in vitro

the major metabolite (r,s)-m-1, and m-1 enantiomers of sarpogrelate specifically blocked 5-ht at 5-ht2a receptors. the stereochemical configuration of the ligands does not obviously play a key role at binding to the 5-ht2a receptor [2].

in vivo

pad patients were divided into two groups. one group treated with 100 mg sarpogrelate in oral 3 times one day for 12 weeks (n = 10), while the other group who remained on conventional therapy as control group (n = 11). forearm blood flow (fbf) and leg blood flow (lbf) responses to reactive hyperemia (rh) and sublingual administration of nitroglycerin (ntg) were measured by strain-gauge plethysmography. after twelve weeks of its administration, fbf and lbf responses during rh exhibited significant increases from 13.2 6 1.7 to 18.1 6 2.2 ml/min every 100 ml tissue (p , 0.01) and from 8.2 6 0.9 to 14.2 6 2.1 ml/min every 100 ml tissue (p , 0.05), respectively. augmentation of fbf and lbf induced by sarpogrelate responses to rh was maintained at 24 weeks. the control group had no change observed in at each follow-up time point. the changes in fbf and lbf after sublingual ntg were similar during follow-up periods in the two groups. these findings suggest that longterm oral administration of sarpogrelate improves vascular function in patients with pad [3].

storage

Desiccate at RT

References

[1] nishio h1, inoue a, nakata y. binding affinity of sarpogrelate, a new antiplatelet agent, and its metabolite for serotonin receptor subtypes. arch int pharmacodyn ther. 1996 mar-apr;331(2):189-202.
[2] pertz h1, elz s. in-vitro pharmacology of sarpogrelate and the enantiomers of its major metabolite: 5-ht2a receptor specificity, stereoselectivity and modulation of ritanserin-induced depression of 5-ht contractions in rat tail artery. j pharm pharmacol. 1995 apr;47(4):310-6.
[3] miyazaki m1, higashi y, goto c, chayama k, yoshizumi m, sanada h, orihashi k, sueda t. sarpogrelate hydrochloride, a selective 5-ht2a antagonist, improves vascular function in patients with peripheral arterial disease. j cardiovasc pharmacol. 2007 apr;49(4):221-7.

Sarpogrelate hydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Sarpogrelate hydrochloride manufacturers

Dideu Industries Group Limited
Product
Sarpogrelate hydrochloride 135159-51-2
Price
US $1.10/g
Min. Order
1g
Purity
99.9%
Supply Ability
100 Tons min
Release date
2021-08-04
Career Henan Chemical Co
Product
Sarpogrelate hydrochloride 135159-51-2
Price
US $3.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
100kg
Release date
2019-08-07
Career Henan Chemical Co
Product
7-AMCA 24701-69-7
Price
US $3.00/ASSAYS
Min. Order
1ASSAYS
Purity
99%
Supply Ability
100kg
Release date
2019-08-06

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