ChemicalBook > CAS DataBase List > MK 0524

MK 0524

Product Name: MK 0524
CAS No.: 571170-77-9
Chemical Name: MK 0524
Synonyms: CS-623;MK 0524;Cardaptive;Laropiprant;Laropiprant, >=99%;Laropiprant(MK0524);MK-0524(Laropiprant)/;MK0524;LAROPIPRANT;MK-0524;Laropiprant, 10 mM in DMSO;[(3R)-4-(4-chlorobenzyl)-7-fluoro-5-(Methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]acetic acid
CBNumber: CB71872243
Molecular Formula: C21H19ClFNO4S
Formula Weight: 435.9
MOL File: 571170-77-9.mol

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MK 0524 Property

Melting point:: 175∶C
Boiling point:: 710.0±60.0 °C(Predicted)
Density: 1.48
storage temp.: Sealed in dry,Store in freezer, under -20°C
solubility: DMSO:20.0(Max Conc. mg/mL);45.88(Max Conc. mM)
DMF:20.0(Max Conc. mg/mL);45.88(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.45(Max Conc. mM)
Ethanol:5.0(Max Conc. mg/mL);11.47(Max Conc. mM)
form: Powder
pka: 4.54±0.10(Predicted)
color: White to off-white

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML3572
Product name: MK-0524
Purity: ≥98% (HPLC)
Packaging: 5 mg
Price: $96.9
Updated: 2025/07/31

Sigma-Aldrich

Product number: SML3572
Product name: MK-0524
Purity: ≥98% (HPLC)
Packaging: 25 mg
Price: $410
Updated: 2025/07/31

Cayman Chemical

Product number: 10009835
Product name: MK-0524
Purity: ≥98%
Packaging: 1mg
Price: $57
Updated: 2024/03/01

Cayman Chemical

Product number: 10009835
Product name: MK-0524
Purity: ≥98%
Packaging: 5mg
Price: $139
Updated: 2024/03/01

Cayman Chemical

Product number: 10009835
Product name: MK-0524
Purity: ≥98%
Packaging: 10mg
Price: $249
Updated: 2024/03/01

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MK 0524 Chemical Properties,Usage,Production

Uses

Laropiprant is a potent and selective DP receptor antagonist with Ki values of 0.57 nM and 2.95 nM for DP receptor and TP Receptor, respectively[1][2][3].

Definition

ChEBI: Laropiprant is an indolyl carboxylic acid.

Biological Activity

MK-0524 is a potent and selective prostaglandin D2 (PGD2) receptor PTGDR (DP1) antagonist with inverse agonist activity (Ki = 570 pM/DP1, 2.95 nM/TP, 745 nM/DP2, >890 nM for EP1/2/3/4, FP and IP). MK-0524 inhibits cAMP accumulation in PGD2-challenged human platelets (IC50 = 90 pM) and blocks PGD2-induced nasal congestion in a sheep allergic rhinitis model in vivo (by 99% at 0.1 mg/kg i.v.). MK-0524 decreases DP1-dependent basal cAMP level in HEK293 (1-100 nM) without affecting DP1-dependent basal ERK1/2 phosphorylation (up to 1 μM).

in vivo

Laropiprant (0-100 mg/kg; p.o. and i.v.; male Sprague-Dawley rats) exhibits good pharmacokinetic profiles^[3].

Pharmacokinetic Analysis in Male Sprague-Dawley rats^[3]

Route	Dose (mg/kg)	AUC_0-∞ (μM·hr)	Cl_p (mL/min/kg)	V_dss (L/kg)	T_1/2 (hr)
PO	1	22.7	1.9	0.7	7.4
PO	5	96.0	2.1	0.9	7.6
Route	Dose (mg/kg)	AUC_0-∞ (μM·hr)	C_max (μM)	T_max (hr)	F(%)
IV	5	52.6	15.6	1.2	/

IC 50

DP: 0.57 nM (Ki); TP Receptor: 2.95 nM (Ki)

storage

Store at -20°C

References

[1] Labrecque P, et, al. Inverse agonist and pharmacochaperone properties of MK-0524 on the prostanoid DP1 receptor. PLoS One. 2013 Jun 10;8(6):e65767.
[2] Sturino CF, et, al. Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524). J Med Chem. 2007 Feb 22;50(4):794-806. DOI:10.1021/jm0603668
[3] Chang SW, et, al. The pharmacokinetics and disposition of MK-0524, a Prosglandin D2 Receptor 1 antagonist, in rats, dogs and monkeys. Xenobiotica. 2007 May;37(5):514-33. DOI:10.1080/00498250601175565

MK 0524 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from MK 0524 manufacturers

Career Henan Chemical Co

Product: Laropiprant 571170-77-9
Price: US $1.00/g
Min. Order: 1g
Purity: 99%
Supply Ability: 1ton
Release date: 2020-01-10

571170-77-9, MK 0524Related Search:

CYCLOPENT[B]INDOLE, 7-FLUORO-1,2,3,4-TETRAHYDRO- MK 0524

Cyclopent[b]indole-3-acetic acid, 4-[(4-chlorophenyl)methyl]-7-fluoro-1,2,3,4-tetrahydro-5-(methylsulfonyl)-, (3R)-Laropiprant

MK 0524

Laropiprant

MK-0524(Laropiprant)/

Laropiprant(MK0524)

(3R)-4-[(4-Chlorophenyl)methyl]-7-fluoro-1,2,3,4-tetrahydro-5-(methylsulfonyl)cyclopent[b]indole-3-acetic acid

[(3R)-4-(4-chlorobenzyl)-7-fluoro-5-(Methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]acetic acid

(R)-2-(4-(4-chlorobenzyl)-7-fluoro-5-(Methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid

Cardaptive

(3R)-4-[(4-Chlorophenyl)methyl]-7-fluoro-1,2,3,4-tetrahydro-5-(methylsulfonyl)cyclopent[b]indole-3-acetic acid Laropiprant MK 0524

Laropiprant, >=99%

MK0524;LAROPIPRANT;MK-0524

CS-623

Cyclopent[b]indole-3-acetic acid, 4-[(4-chlorophenyl)methyl]-7-fluoro-1,2,3,4-tetrahydro-5-(methylsulfonyl)-, (3R)-

Laropiprant, 10 mM in DMSO

571170-77-9

C21H19ClFNO4S