2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. LY2119620

LY2119620 is a high-affinity muscarinic M2/M4 receptor agonist.

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LY2119620

LY2119620 構造式

CAS 番号 : 886047-22-9

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 169 在庫あり
Solution
10 mM * 1 mL in DMSO USD 169 在庫あり
Solid
5 mg $154 在庫あり
10 mg $242 在庫あり
25 mg $418 在庫あり
50 mg $585 在庫あり
100 mg $820 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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LY2119620 関連抗体

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mAChR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

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製品説明

LY2119620 is a high-affinity muscarinic M2/M4 receptor agonist.

IC50 & Target

mAChR2

 

mAChR4

 

体外実験

LY2119620 shows a modest allosteric agonism of 23.2±2.18% and 16.8±5.01% at the M2 and M4 receptors, respectively. Minimal allosteric agonism (<20%) is observed for LY2119620 at the M1, M3, and M5 receptors. The variable KB of LY2119620 for the allosteric binding site on the unoccupied receptor is found to be consistently about 1.9 to 3.4 μM. Results show a Bmax increase at the M2 receptor from 793±1.95 fmol/mg to 2850±162 fmol/mg upon addition of 10 μM LY2119620, and about a 5-fold increase in Bmax at the M4 receptor, 284±18.3 fmol/mg to 1340±42.2 fmol/mg[1].

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

LY2119620 関連抗体
分子量

437.94

分子式

C19H24ClN5O3S
CAS 番号
Appearance

Solid

Color

White to light yellow

SMILES

NC1=C(C(NC2CC2)=O)SC3=C1C(C)=C(Cl)C(OCC(N4CCN(C)CC4)=O)=N3
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 67.5 mg/mL (154.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2834 mL 11.4171 mL 22.8342 mL
5 mM 0.4567 mL 2.2834 mL 4.5668 mL
10 mM 0.2283 mL 1.1417 mL 2.2834 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. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

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体積 （終了）

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.71 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.71 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.74%

COA (247 KB) HNMR (184 KB) LCMS (343 KB)

取扱説明書 (2659 KB)
参考文献
キナーゼ実験
[1]

[3H]LY2119620 equilibrium binding is achieved by incubating 15 µg membranes, orthosteric ligand (100 µM), and various concentrations of [3H]LY2119620 (0.2 to 60 nM) for 1 hour at 25°C. The specific binding versus time data are fit to a one-site specific binding model, and the Bmax and Kd for the allosteric molecule are calculated for each orthosteric ligand[1].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

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. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2834 mL 11.4171 mL 22.8342 mL 57.0854 mL
5 mM 0.4567 mL 2.2834 mL 4.5668 mL 11.4171 mL
10 mM 0.2283 mL 1.1417 mL 2.2834 mL 5.7085 mL
15 mM 0.1522 mL 0.7611 mL 1.5223 mL 3.8057 mL
20 mM 0.1142 mL 0.5709 mL 1.1417 mL 2.8543 mL
25 mM 0.0913 mL 0.4567 mL 0.9134 mL 2.2834 mL
30 mM 0.0761 mL 0.3806 mL 0.7611 mL 1.9028 mL
40 mM 0.0571 mL 0.2854 mL 0.5709 mL 1.4271 mL
50 mM 0.0457 mL 0.2283 mL 0.4567 mL 1.1417 mL
60 mM 0.0381 mL 0.1903 mL 0.3806 mL 0.9514 mL
80 mM 0.0285 mL 0.1427 mL 0.2854 mL 0.7136 mL
100 mM 0.0228 mL 0.1142 mL 0.2283 mL 0.5709 mL
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LY2119620 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LY2119620886047-22-9LY 2119620LY-2119620mAChRMuscarinic acetylcholine receptorInhibitorinhibitorinhibit

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製品名:
LY2119620
製品番号:
HY-15885
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