الصفحة الرئيسية>>Signaling Pathways>> Proteases>> Ser/Thr Protease>>PF-06446846 hydrochloride

PF-06446846 hydrochloride

رقم الكتالوجGC38028

هيدروكلوريد PF-06446846 هو مثبط فعال عن طريق الفم وانتقائي للغاية لترجمة Proprotein convertase subtilisin / kexin type 9 (PCSK9)

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PF-06446846 hydrochloride التركيب الكيميائي

Cas No.: 1632250-50-0

الحجم السعر المخزون الكميّة
1mg
92٫00
متوفر
5mg
255٫00
متوفر
10mg
408٫00
متوفر
25mg
663٫00
متوفر
50mg
1224٫00
متوفر
100mg
2141٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of PF-06446846 hydrochloride

PF-06446846 hydrochloride is an orally active and highly selective inhibitor of translation of Proprotein convertase subtilisin/kexin type 9 (PCSK9). PF-06446846 hydrochloride inhibits PCSK9 by inducing the ribosome to stall around codon 34[1].

PF-06446846 inhibits the secretion of PCSK9 by Huh7 cells with an IC50 of 0.3 μM[1].

PF-06446846 (oral gavage; 5-50 mg/kg/day for 14 days) lowers plasma PCSK9 in a dose-dependent manner and lowers total cholesterol levels[1]. Animal Model: Male Sprague-Dawley (Crl:CD [SD] rats, 6-8 wk old at initiation of dosing)[1]

[1]. Lintner NG, et al. Selective stalling of human translation through small-molecule engagement of the ribosome nascent chain. PLoS Biol. 2017 Mar 21;15(3):e2001882.

Chemical Properties of PF-06446846 hydrochloride

Cas No. 1632250-50-0 SDF
Canonical SMILES O=C(N(C1=NC=CC=C1Cl)[C@H]2CNCCC2)C3=CC=C(N4N=NC5=CC=CN=C54)C=C3.[H]Cl.[x]
Formula C22H20ClN7O.xHCl M.Wt
الذوبان DMSO : 250 mg/mL (531.52 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.
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In vivo Formulation Calculator (Clear solution) of PF-06446846 hydrochloride

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

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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.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Review for PF-06446846 hydrochloride

Average Rating: 5 ★★★★★ (Based on Reviews and 33 reference(s) in Google Scholar.)

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