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Finasteride 5-alpha Reductase inhibitor

Name: Finasteride
Brand: Selleck Chemicals
SKU: S1197
Availability: InStock
Rating: 5 (9 reviews)

Cat.No.S1197

Finasteride (MK-906) is a potent, reversible inhibitor of the rat type 1 5 alpha-reductase with K_i of 10.2 nM, used in the treatment of benign prostatic hyperplasia (BPH) and male pattern baldness (MPB).

Chemical Structure

Molecular Weight: 372.54

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: Purity: 99.89%

99.89

Related Targets	Adrenergic Receptor Estrogen/progestogen Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Opioid Receptor THR PGES Aromatase CCK receptor Mineralocorticoid Receptor GHSR SSTR TSH Receptor GNRH Receptor PGDS
Related Products	Cinchonine(LA40221) Atosiban Terlipressin Acetate Exenatide Acetate (Exendin-4)

Chemical Information, Storage & Stability

Molecular Weight	372.54	Formula	C₂₃H₃₆N₂O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	98319-26-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	MK-906			Smiles	CC12CCC3C(C1CCC2C(=O)NC(C)(C)C)CCC4C3(C=CC(=O)N4)C

Solubility

In vitro
Batch:

DMSO : 75 mg/mL ( (201.32 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 18 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.750mg/ml (10.07mM)	Taking the 1 mL working solution as an example, add 50 μL of 75 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.450mg/ml (1.21mM)	Taking the 1 mL working solution as an example, add 50 μL of 9 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	5-α reductase ^[1] 10.2 nM(Ki)
In vitro	Finasteride binds to the type 2 isozyme-NADPH complex to form a ternary complex with Ki of 1.19 nM, which then rearranges to a high affinity complex (E:I) with a pseudo first order rate constant of 1.62 ms. ^[1] This compound dose-dependently inhibits the growth rate of the LnCap cell line. ^[2] It markedly inhibits prostate-specific antigen (PSA) secretion and expression in LNCaP cells. ^[3]
In vivo	Finasteride induces dosage-related incidences of hypospadias (penischisis) in male offspring with a threshold dosage level near 0.1 mg/kg/day and a 100% effect level of 100 mg/kg/day in male rats. This compound also causes decreased anogenital distance in male offspring in male rats. ^[4] This chemical and castration decreases prostate weight at day 21 by 65% and 93%, respectively, in rats. It has no significant effect on DNA content after 4 days and decreases DNA content by a maximum of 52% at 14 days in rats. It causes a less intense increase in staining in which 16% of epithelial cells stained for tissue transglutaminase on day 9 with a return to baseline by day 14 in rats. This compound-induced staining is less intense with peak staining at day 4 (0.7% of epithelial cells) and a return to control values by day 9 in rats. ^[5]
References	https://pubmed.ncbi.nlm.nih.gov/9328210/ https://pubmed.ncbi.nlm.nih.gov/7855976/ https://pubmed.ncbi.nlm.nih.gov/9044850/ https://pubmed.ncbi.nlm.nih.gov/2168096/ https://pubmed.ncbi.nlm.nih.gov/7835306/ https://pubmed.ncbi.nlm.nih.gov/9066407/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04288427	Recruiting	Benign Prostatic Hyperplasia\|Prostate Hyperplasia\|Prostate Disease\|Prostate Hypertrophy\|Prostate Pain\|Lower Urinary Tract Symptoms\|Urinary Obstruction\|Urinary Tract Disease	Beth Israel Deaconess Medical Center\|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)	September 25 2020	Not Applicable
NCT03669692	Withdrawn	Prostatic Hyperplasia Benign\|Metabolic Syndrome	Complexo Hospitalario Universitario de A Coruña	July 10 2018	Not Applicable
NCT02824380	Completed	Androgenic Alopecia	Dong-A ST Co. Ltd.	July 2016	Phase 1
NCT02146937	Withdrawn	Detectable Prostate Nodules	Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins	March 2014	Phase 2
NCT01703520	Completed	Male Breast Cancer	Organon and Co\|Institute for Applied Economics and Health Research Aps	May 1 2011	--

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