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MedKoo Cat#: 565339 | Name: PCSK9 Modulator

Description:

WARNING: This product is for research use only, not for human or veterinary use.

PCSK9 modulator is a modulator of proprotein convertase subtilisin kexin like type 9 (PCSK9).

Chemical Structure

PCSK9 Modulator
PCSK9 Modulator
CAS#NONE

Theoretical Analysis

MedKoo Cat#: 565339

Name: PCSK9 Modulator

CAS#: NONE

Chemical Formula: C15H6ClF6NO

Exact Mass: 365.0042

Molecular Weight: 365.66

Elemental Analysis: C, 49.27; H, 1.65; Cl, 9.69; F, 31.17; N, 3.83; O, 4.38

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
PCSK9 modulator
IUPAC/Chemical Name
7-Chloro-6-(trifluoromethyl)-2-(4-(trifluoromethyl)phenyl)benzo[d]oxazole
InChi Key
SIKMFPAJZVLOEM-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H6ClF6NO/c16-11-9(15(20,21)22)5-6-10-12(11)24-13(23-10)7-1-3-8(4-2-7)14(17,18)19/h1-6H
SMILES Code
FC(C1=CC=C(C2=NC3=CC=C(C(F)(F)F)C(Cl)=C3O2)C=C1)(F)F
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 365.66 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Elseweidy MM, Elswefy SE, Younis NN, Tarek S. Contribution of aorta glycosaminoglycans and PCSK9 to hyperlipidemia in experimental rabbits: the role of 10-dehdrogingerdione as effective modulator. Mol Biol Rep. 2019 May 2. doi: 10.1007/s11033-019-04836-1. [Epub ahead of print] PubMed PMID: 31049833. 2: Tang ZH, Li TH, Peng J, Zheng J, Li TT, Liu LS, Jiang ZS, Zheng XL. PCSK9: A novel inflammation modulator in atherosclerosis? J Cell Physiol. 2019 Mar;234(3):2345-2355. doi: 10.1002/jcp.27254. Epub 2018 Sep 24. Review. PubMed PMID: 30246446. 3: Bandyopadhyay D, Ashish K, Hajra A, Qureshi A, Ghosh RK. Cardiovascular Outcomes of PCSK9 Inhibitors: With Special Emphasis on Its Effect beyond LDL-Cholesterol Lowering. J Lipids. 2018 Mar 25;2018:3179201. doi: 10.1155/2018/3179201. eCollection 2018. Review. PubMed PMID: 29770231; PubMed Central PMCID: PMC5889852. 4: Pettersen D, Fjellström O. Small molecule modulators of PCSK9 - A literature and patent overview. Bioorg Med Chem Lett. 2018 Apr 15;28(7):1155-1160. doi: 10.1016/j.bmcl.2018.02.046. Epub 2018 Feb 26. Review. PubMed PMID: 29519739. 5: Camera M, Rossetti L, Barbieri SS, Zanotti I, Canciani B, Trabattoni D, Ruscica M, Tremoli E, Ferri N. PCSK9 as a Positive Modulator of Platelet Activation. J Am Coll Cardiol. 2018 Feb 27;71(8):952-954. doi: 10.1016/j.jacc.2017.11.069. PubMed PMID: 29471945. 6: Ghosh Laskar M, Eriksson M, Rudling M, Angelin B. Treatment with the natural FXR agonist chenodeoxycholic acid reduces clearance of plasma LDL whilst decreasing circulating PCSK9, lipoprotein(a) and apolipoprotein C-III. J Intern Med. 2017 Jun;281(6):575-585. doi: 10.1111/joim.12594. Epub 2017 Feb 1. PubMed PMID: 28145001. 7: He NY, Li Q, Wu CY, Ren Z, Gao Y, Pan LH, Wang MM, Wen HY, Jiang ZS, Tang ZH, Liu LS. Lowering serum lipids via PCSK9-targeting drugs: current advances and future perspectives. Acta Pharmacol Sin. 2017 Mar;38(3):301-311. doi: 10.1038/aps.2016.134. Epub 2017 Jan 23. Review. PubMed PMID: 28112180; PubMed Central PMCID: PMC5342665. 8: Thiery J, Burkhardt R. [PCSK9 - "missing link" in familial hypercholesterolemia : New therapeutic options in hypercholesterolemia and coronary artery disease]. Herz. 2016 Jun;41(4):281-9. doi: 10.1007/s00059-016-4435-3. Review. German. PubMed PMID: 27215417. 9: Kysenius K, Huttunen HJ. Stress-induced upregulation of VLDL receptor alters Wnt-signaling in neurons. Exp Cell Res. 2016 Jan 15;340(2):238-47. doi: 10.1016/j.yexcr.2016.01.001. Epub 2016 Jan 2. PubMed PMID: 26751967. 10: Si-Tayeb K, Idriss S, Champon B, Caillaud A, Pichelin M, Arnaud L, Lemarchand P, Le May C, Zibara K, Cariou B. Urine-sample-derived human induced pluripotent stem cells as a model to study PCSK9-mediated autosomal dominant hypercholesterolemia. Dis Model Mech. 2016 Jan;9(1):81-90. doi: 10.1242/dmm.022277. Epub 2015 Nov 19. PubMed PMID: 26586530; PubMed Central PMCID: PMC4728336. 11: Pirillo A, Catapano AL. Berberine, a plant alkaloid with lipid- and glucose-lowering properties: From in vitro evidence to clinical studies. Atherosclerosis. 2015 Dec;243(2):449-61. doi: 10.1016/j.atherosclerosis.2015.09.032. Epub 2015 Sep 30. Review. PubMed PMID: 26520899. 12: Basu D, Huq A, Iqbal J, Hussain MM, Jiang XC, Jin W. Hepatic S1P deficiency lowers plasma cholesterol levels in apoB-containing lipoproteins when LDLR function is compromised. Nutr Metab (Lond). 2015 Oct 20;12:35. doi: 10.1186/s12986-015-0031-4. eCollection 2015. PubMed PMID: 26495026; PubMed Central PMCID: PMC4613744. 13: Yang JH, Bang MA, Jang CH, Jo GH, Jung SK, Ki SH. Alginate oligosaccharide enhances LDL uptake via regulation of LDLR and PCSK9 expression. J Nutr Biochem. 2015 Nov;26(11):1393-400. doi: 10.1016/j.jnutbio.2015.07.009. Epub 2015 Jul 30. PubMed PMID: 26320675. 14: Hong C, Marshall SM, McDaniel AL, Graham M, Layne JD, Cai L, Scotti E, Boyadjian R, Kim J, Chamberlain BT, Tangirala RK, Jung ME, Fong L, Lee R, Young SG, Temel RE, Tontonoz P. The LXR-Idol axis differentially regulates plasma LDL levels in primates and mice. Cell Metab. 2014 Nov 4;20(5):910-918. doi: 10.1016/j.cmet.2014.10.001. Epub 2014 Nov 4. PubMed PMID: 25440061; PubMed Central PMCID: PMC4261644. 15: Chorba JS, Shokat KM. The proprotein convertase subtilisin/kexin type 9 (PCSK9) active site and cleavage sequence differentially regulate protein secretion from proteolysis. J Biol Chem. 2014 Oct 17;289(42):29030-43. doi: 10.1074/jbc.M114.594861. Epub 2014 Sep 10. PubMed PMID: 25210046; PubMed Central PMCID: PMC4200258. 16: Norata GD, Tibolla G, Catapano AL. PCSK9 inhibition for the treatment of hypercholesterolemia: promises and emerging challenges. Vascul Pharmacol. 2014 Aug;62(2):103-11. doi: 10.1016/j.vph.2014.05.011. Epub 2014 Jun 9. Review. PubMed PMID: 24924410. 17: Seidah NG, Awan Z, Chrétien M, Mbikay M. PCSK9: a key modulator of cardiovascular health. Circ Res. 2014 Mar 14;114(6):1022-36. doi: 10.1161/CIRCRESAHA.114.301621. Review. PubMed PMID: 24625727. 18: Lambert G, Jarnoux AL, Pineau T, Pape O, Chetiveaux M, Laboisse C, Krempf M, Costet P. Fasting induces hyperlipidemia in mice overexpressing proprotein convertase subtilisin kexin type 9: lack of modulation of very-low-density lipoprotein hepatic output by the low-density lipoprotein receptor. Endocrinology. 2006 Oct;147(10):4985-95. Epub 2006 Jun 22. PubMed PMID: 16794006.