PF-06446846 (hydrochloride)

Name: PF-06446846 hydrochloride
Brand: MedChemExpress
SKU: HY-120088A
Rating: 5.0 (6 reviews)

製品番号: HY-120088A 純度: 99.44%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

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.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

PF-06446846 (hydrochloride) 構造式

CAS 番号 : 1632250-50-0

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 155	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 155	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$150	在庫あり	Estimated Time of Arrival: December 31
10 mg	$255	在庫あり	Estimated Time of Arrival: December 31
25 mg	$600	在庫あり	Estimated Time of Arrival: December 31
50 mg	$900	在庫あり	Estimated Time of Arrival: December 31
100 mg	$1350	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 6 publication(s) in Google Scholar

Other Forms of PF-06446846 hydrochloride:

PF-06446846 在庫あり

顧客検証

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•関連小分子:

•関連タンパク質:

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

PCSK9^[1]

体外実験

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague-Dawley (Crl:CD [SD] rats, 6-8 wk old at initiation of dosing)^[1]
Dosage:	5, 15, and 50 mg/kg
Administration:	Oral gavage; daily for 14 days
Result:	Lowered plasma PCSK9 in a dose-dependent manner and lowered total cholesterol levels.

分子量

470.35

分子式

C₂₂H₂₁Cl₂N₇O

CAS 番号

1632250-50-0

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N(C1=NC=CC=C1Cl)[C@H]2CNCCC2)C3=CC=C(N4N=NC5=CC=CN=C54)C=C3.[H]Cl

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (212.61 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 100 mg/mL (212.61 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1261 mL	10.6304 mL	21.2608 mL
5 mM	0.4252 mL	2.1261 mL	4.2522 mL
10 mM	0.2126 mL	1.0630 mL	2.1261 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (10.63 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (10.63 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 100 mg/mL (212.61 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

純度とドキュメンテーション

純度: 99.44%

Select Batch:

データシート (277 KB) SDS (393 KB)

COA (254 KB) HNMR (311 KB) LCMS (95 KB)

取扱説明書 (2659 KB)

参考文献

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	2.1261 mL	10.6304 mL	21.2608 mL	53.1519 mL
	5 mM	0.4252 mL	2.1261 mL	4.2522 mL	10.6304 mL
	10 mM	0.2126 mL	1.0630 mL	2.1261 mL	5.3152 mL
	15 mM	0.1417 mL	0.7087 mL	1.4174 mL	3.5435 mL
	20 mM	0.1063 mL	0.5315 mL	1.0630 mL	2.6576 mL
	25 mM	0.0850 mL	0.4252 mL	0.8504 mL	2.1261 mL
	30 mM	0.0709 mL	0.3543 mL	0.7087 mL	1.7717 mL
	40 mM	0.0532 mL	0.2658 mL	0.5315 mL	1.3288 mL
	50 mM	0.0425 mL	0.2126 mL	0.4252 mL	1.0630 mL
	60 mM	0.0354 mL	0.1772 mL	0.3543 mL	0.8859 mL
	80 mM	0.0266 mL	0.1329 mL	0.2658 mL	0.6644 mL
	100 mM	0.0213 mL	0.1063 mL	0.2126 mL	0.5315 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.