MedKoo Cat#: 463509 | Name: Gemfibrozil-d6
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Description:

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

Gemfibrozil-d6 is intended for use as an internal standard for the quantification of gemfibrozil by GC- or LC-MS. Gemfibrozil is a peroxisome proliferator-activated reporter α and PPARγ agonist. In vivo, gemfibrozil reduces serum total cholesterol, triglyceride, and LDL levels in a rat model of high-cholesterol diet-induced hyperlipidemia. Gemfibrozil reduces atherosclerotic plaque area, superoxide production, and expression of the genes encoding the NF-κB subunit p65 and chemokine (C-C) motif ligand 2 (CCL2) in ApoE-/- mice. Formulations containing gemfibrozil have been used in the treatment of high cholesterol.

Chemical Structure

Gemfibrozil-d6
Gemfibrozil-d6
CAS#1184986-45-5

Theoretical Analysis

MedKoo Cat#: 463509

Name: Gemfibrozil-d6

CAS#: 1184986-45-5

Chemical Formula: C15H16D6O3

Exact Mass: 256.1946

Molecular Weight: 256.37

Elemental Analysis: C, 70.27; H, 11.00; O, 18.72

Price and Availability

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1mg USD 350.00 2 Weeks
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Synonym
Gemfibrozil-d6; Gemfibrozild6; Gemfibrozil d6; CI-719-d6; CI719-d6; CI 719-d6; CI-719 d6; CI-719d6; CI719d6; CI 719 d6;
IUPAC/Chemical Name
5-(2,5-dimethylphenoxy)-2,2-bis(methyl-d3)pentanoic acid
InChi Key
HEMJJKBWTPKOJG-LIJFRPJRSA-N
InChi Code
InChI=1S/C15H22O3/c1-11-6-7-12(2)13(10-11)18-9-5-8-15(3,4)14(16)17/h6-7,10H,5,8-9H2,1-4H3,(H,16,17)/i3D3,4D3
SMILES Code
OC(C(C([2H])([2H])[2H])(CCCOC1=C(C)C=CC(C)=C1)C([2H])([2H])[2H])=O
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
Product Data
Biological target:
Gemfibrozil-d6 (CI-719-d6) is the deuterium labeled Gemfibrozil. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering drug; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
In vitro activity:
The level of cellular TG (triglycerides) was detected and was observed to be decreased by 43.8% at 50 µM GEM (gemfibrozil) compared with cells treated with 1 mM OA only (Fig. 2C). To further confirm the lipid changes in the cellular model, TLC analysis was performed. TLC results suggested that there was a decrease in TG levels in cells treated with 50 µM GEM compared with those treated with OA only (Fig. 2D). Taken together, GEM may lower the lipid accumulation in an in vitro model of NAFLD. The optimal concentration is 50 µM. Reference: Exp Ther Med. 2019 Feb;17(2):1282-1289. https://pubmed.ncbi.nlm.nih.gov/30680004/
In vivo activity:
Finally, this study found that animals in the gemfibrozil treatment group showed significant improvement in locomotive activity (Fig. 1J), and in the frequency of supported rearing (Fig. 1L) and grooming (Fig. 1M), indicating a functional improvement in activities mediated by the striatum. In addition, treatment with gemfibrozil significantly improved motor coordination as measured by rotarod (Fig. 1K). Together, these results suggest that gemfibrozil protects the nigrostriatum and improves locomotor activities in the MPTP mouse model of PD. Reference: J Neurosci. 2021 Mar 10;41(10):2287-2300. https://pubmed.ncbi.nlm.nih.gov/33514677/

Preparing Stock Solutions

The following data is based on the product molecular weight 256.37 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
Formulation protocol:
1. Zhang X, Wang S, Hu L, Wang J, Liu Y, Shi P. Gemfibrozil reduces lipid accumulation in SMMC-7721 cells via the involvement of PPARα and SREBP1. Exp Ther Med. 2019 Feb;17(2):1282-1289. doi: 10.3892/etm.2018.7046. Epub 2018 Dec 5. PMID: 30680004; PMCID: PMC6327679. 2. Pahan K, Jana M, Liu X, Taylor BS, Wood C, Fischer SM. Gemfibrozil, a lipid-lowering drug, inhibits the induction of nitric-oxide synthase in human astrocytes. J Biol Chem. 2002 Nov 29;277(48):45984-91. doi: 10.1074/jbc.M200250200. Epub 2002 Sep 18. PMID: 12244038; PMCID: PMC2045648. 3. Gottschalk CG, Jana M, Roy A, Patel DR, Pahan K. Gemfibrozil Protects Dopaminergic Neurons in a Mouse Model of Parkinson's Disease via PPARα-Dependent Astrocytic GDNF Pathway. J Neurosci. 2021 Mar 10;41(10):2287-2300. doi: 10.1523/JNEUROSCI.3018-19.2021. Epub 2021 Jan 29. PMID: 33514677; PMCID: PMC8018777. 4. Shields CA, Poudel B, McPherson KC, Brown AK, Ekperikpe US, Browning E, Sutton L, Cornelius DC, Williams JM. Treatment With Gemfibrozil Prevents the Progression of Chronic Kidney Disease in Obese Dahl Salt-Sensitive Rats. Front Physiol. 2020 Sep 18;11:566403. doi: 10.3389/fphys.2020.566403. PMID: 33071820; PMCID: PMC7533555.
In vitro protocol:
1. Zhang X, Wang S, Hu L, Wang J, Liu Y, Shi P. Gemfibrozil reduces lipid accumulation in SMMC-7721 cells via the involvement of PPARα and SREBP1. Exp Ther Med. 2019 Feb;17(2):1282-1289. doi: 10.3892/etm.2018.7046. Epub 2018 Dec 5. PMID: 30680004; PMCID: PMC6327679. 2. Pahan K, Jana M, Liu X, Taylor BS, Wood C, Fischer SM. Gemfibrozil, a lipid-lowering drug, inhibits the induction of nitric-oxide synthase in human astrocytes. J Biol Chem. 2002 Nov 29;277(48):45984-91. doi: 10.1074/jbc.M200250200. Epub 2002 Sep 18. PMID: 12244038; PMCID: PMC2045648.
In vivo protocol:
1. Gottschalk CG, Jana M, Roy A, Patel DR, Pahan K. Gemfibrozil Protects Dopaminergic Neurons in a Mouse Model of Parkinson's Disease via PPARα-Dependent Astrocytic GDNF Pathway. J Neurosci. 2021 Mar 10;41(10):2287-2300. doi: 10.1523/JNEUROSCI.3018-19.2021. Epub 2021 Jan 29. PMID: 33514677; PMCID: PMC8018777. 2. Shields CA, Poudel B, McPherson KC, Brown AK, Ekperikpe US, Browning E, Sutton L, Cornelius DC, Williams JM. Treatment With Gemfibrozil Prevents the Progression of Chronic Kidney Disease in Obese Dahl Salt-Sensitive Rats. Front Physiol. 2020 Sep 18;11:566403. doi: 10.3389/fphys.2020.566403. PMID: 33071820; PMCID: PMC7533555.