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Laropiprant

Laropiprant

  • CAT Number: I004130
  • CAS Number: 571170-77-9
  • Molecular Formula: C21H19ClFNO4S
  • Molecular Weight: 435.9
  • Purity: ≥95%
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Laropiprant (CAT: I004130) is a selective antagonist of the prostaglandin D2 receptor subtype 1 (DP1 receptor). It is primarily used in combination with niacin (nicotinic acid) to reduce the flushing side effects associated with niacin therapy. Flushing is a common side effect of niacin, characterized by redness, warmth, and itching of the skin. Laropiprant acts by blocking the DP1 receptor, which is involved in the vasodilation and flushing response triggered by niacin. By inhibiting DP1 receptor activation, laropiprant helps to reduce niacin-induced flushing, making niacin therapy more tolerable for patients.

Catalog Number I004130
CAS Number 571170-77-9
Molecular Formula

C21H19ClFNO4S

Purity 95%
Target DP1 receptor
Solubility 10 mM in DMSO
Storage Store at -20°C
IC50 0.57 nM/0.75 uM (Ki for DP1/DP2)
InChI InChI=1S/C21H19ClFNO4S/c1-29(27,28)18-10-15(23)9-17-16-7-4-13(8-19(25)26)20(16)24(21(17)18)11-12-2-5-14(22)6-3-12/h2-3,5-6,9-10,13H,4,7-8,11H2,1H3,(H,25,26)/t13-/m1/s1
InChIKey NXFFJDQHYLNEJK-CYBMUJFWSA-N
SMILES FC1=CC2=C(N(CC3=CC=C(Cl)C=C3)C4=C2CC[C@@H]4CC(O)=O)C(S(C)(=O)=O)=C1
Reference

<br />
1:Effects of Vascular and Nonvascular Adverse Events and of Extended-Release Niacin With Laropiprant on Health and Healthcare Costs. Kent S, Haynes R, Hopewell JC, Parish S, Gray A, Landray MJ, Collins R, Armitage J, Mihaylova B; HPS2-THRIVE Collaborative Group..Circ Cardiovasc Qual Outcomes. 2016 Jul;9(4):348-54. doi: 10.1161/CIRCOUTCOMES.115.002592. Epub 2016 Jul 12. PMID: 27407053 <br />
2:Effects of extended-release niacin/laropiprant on correlations between apolipoprotein B, LDL-cholesterol and non-HDL-cholesterol in patients with type 2 diabetes. Brinton EA, Triscari J, Brudi P, Chen E, Johnson-Levonas AO, Sisk CM, Ruck RA, MacLean AA, Maccubbin D, Mitchel YB.Lipids Health Dis. 2016 Jul 12;15(1):116. doi: 10.1186/s12944-016-0282-8. PMID: 27405296 Free PMC Article<br />
3:Extended-Release Niacin/Laropiprant Improves Overall Efficacy of Postprandial Reverse Cholesterol Transport. El Khoury P, Waldmann E, Huby T, Gall J, Couvert P, Lacorte JM, Chapman J, Frisdal E, Lesnik P, Parhofer KG, Le Goff W, Guerin M.Arterioscler Thromb Vasc Biol. 2016 Feb;36(2):285-94. doi: 10.1161/ATVBAHA.115.306834. Epub 2015 Dec 17. PMID: 26681758 Free Article<br />
4:Detrimental effects of niacin/laropiprant on microvascular reactivity and red cell deformability in patients with elevated lipoprotein(a) levels. Cioni G, Mannini L, Liotta AA, D/’Alessandri G, Fatini C, Bandinelli B, Costanzo M, Abbate R, Marcucci R.J Thromb Thrombolysis. 2016 Apr;41(3):433-5. doi: 10.1007/s11239-015-1256-9. PMID: 26289089 <br />
5:Pharmacogenetics of cutaneous flushing response to niacin/laropiprant combination in Hong Kong Chinese patients with dyslipidemia. Hu M, Yang YL, Chan P, Tomlinson B.Pharmacogenomics. 2015;16(12):1387-97. doi: 10.2217/pgs.15.79. Epub 2015 Jul 31. PMID: 26226939 <br />
6:Safety and tolerability of extended-release niacin-laropiprant: Pooled analyses for 11,310 patients in 12 controlled clinical trials. McKenney J, Bays H, Gleim G, Mitchel Y, Kuznetsova O, Sapre A, Sirah W, Maccubbin D.J Clin Lipidol. 2015 May-Jun;9(3):313-25. doi: 10.1016/j.jacl.2015.02.006. Epub 2015 Mar 2. PMID: 26073389 <br />
7:Effect of Extended-Release Niacin/Laropiprant Combination on Plasma Adiponectin and Insulin Resistance in Chinese Patients with Dyslipidaemia. Hu M, Yang YL, Masuda D, Yamashita S, Tomlinson B.Dis Markers. 2015;2015:154014. doi: 10.1155/2015/154014. Epub 2015 Apr 29. PMID: 26063948 Free PMC Article<br />
8:Extended-release niacin/laropiprant significantly improves lipid levels in type 2 diabetes mellitus irrespective of baseline glycemic control. Bays HE, Brinton EA, Triscari J, Chen E, Maccubbin D, MacLean AA, Gibson KL, Ruck RA, Johnson-Levonas AO, O/’Neill EA, Mitchel YB.Vasc Health Risk Manag. 2015 Feb 24;11:165-72. doi: 10.2147/VHRM.S70907. eCollection 2015. PMID: 25750540 Free PMC Article<br />
9:ACP Journal Club: adding niacin plus laropiprant to statins did not reduce vascular events and increased serious adverse events. Bloomfield HE.Ann Intern Med. 2014 Nov 18;161(10):JC8. doi: 10.7326/0003-4819-161-10-201411180-02008. No abstract available. PMID: 25402541 <br />
10:Non-obligatory role of prostaglandin D2 receptor subtype 1 in rosacea: laropiprant in comparison to a placebo did not alleviate the symptoms of erythematoelangiectaic rosacea. Krishna R, Guo Y, Schulz V, Cord-Cruz E, Smith S, Hair S, Nahm WK, Draelos ZD.J Clin Pharmacol. 2015 Feb;55(2):137-43. doi: 10.1002/jcph.383. Epub 2014 Sep 4. PMID: 25142778

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