製品番号: HY-10499

PH-064

(別名: BIM-46187)

2 Cited Publications

カスタマーレビュー

Based on 2 publication(s) in Google Scholar

PH-064 (BIM-46187) is an orally active inhibitor of the heterotrimeric G-protein complex. PH-064 inhibits SERT activity and attenuates shear stress-induced Akt phosphorylation. PH-064 has potent anti-hyperalgesia activity. PH-064 inhibits G protein-coupled receptor-dependent tumorigenesis. PH-064 can be used in the study of pain (e.g., inflammatory pain, neuropathic pain), GPCR-dependent tumors, and inflammatory lung injury.

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純度: 98.78%
CAS 番号: 892546-37-1
分子式: C₄₄H₅₈N₈O₂S₂
分子量:795.11

保管条件:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

PH-064 構造式

CAS 番号: 892546-37-1

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数量

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生物活性
- 製品説明
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (2)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

Akt アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
MP41	IC₅₀	10.2 μM Compound: BIM-46187; 3	Antiproliferative activity against human MP41 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against human MP41 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method	[PMID: 35716516]

体外実験

PH-064 (20 μM; 1 h) abrogates the flow-induced dissociation of Gαq/11 from PECAM-1 in HCAECs and attenuates shear stress-induced Akt phosphorylation^[2].
PH-064 (10 μM-100 μM; 30 min) concentration-dependently inhibits SERT-mediated 5HT uptake in mouse midbrain and frontal cortex synaptosomes, and also inhibits SERT activity in TRex-SERT cells^[3].
PH-064 (for basal IP: even at 10^-4 M) has no inhibitory effect on basal IP production in E151A-CCK2R-transfected COS cells, but completely inhibits Gastrin-stimulated IP production (EC₅₀: 34 μM)^[5].
PH-064 (10 μM; 1 h) reduces IFNγ generation in RGS2 null BMDMs to the level of WT-BMDMs without affecting BMDM viability^[6].

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

体内実験

PH-064 (0.1-1 mg/kg; i.v.) elicits dose-dependent anti-hyperalgesic effect in Carrageenan (HY-125474)-induced hyperalgesia model in rats, without affecting paw oedema and motor performance^[1].
PH-064 (0.3-3 mg/kg; i.v.) shows dose-dependent anti-hyperalgesic effect in chronic constriction injury (CCI) model in rats^[1].
PH-064 (75 mg/kg; p.o.; twice a day; 16 days) exhibits antitumor activity in athymic nude mouse xenografts with E151A-CCK2R-NIH-3T3 cells without apparent toxicity^[5].
PH-064 (3 mg/kg; i.v.; 2 h after i.t. LPS) reduces IFNγ expression by 80% in RGS2 null mouse lungs and promotes resolution of lung edema^[6].

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

Animal Model:

Male Sprague Dawley rats (160-170 g on arrival, allowed to habituate for at least 5 days; Carrageenan-induced hyperalgesia model)^[1]
Dosage:

0.1 mg/kg, 1 mg/kg
Administration:

Intravenous injection
Result:

Significantly increased paw withdrawal thresholds (1 mg/kg: 10 g/40 at 0.5 h, 8.9 g/40 at 2.5 h).

化学情報

CAS 番号 892546-37-1
性状 Solid
分子量 795.11
分子式 C₄₄H₅₈N₈O₂S₂
Color White to light yellow
SMILES

O=C([C@H](CSSC[C@@H](C(N1CCN2C([C@@H]1CC3CCCCC3)=NC(C4=CC=CC=C4)=C2)=O)N)N)N([C@H]5CC6CCCCC6)CCN(C5=N7)C=C7C8=CC=CC=C8
別名

BIM-46187
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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Phytomedicine

Sinapine targeting PLCβ3 EF hands disrupts Gαq-PLCβ3 interaction and ameliorates cardiovascular diseases. [Abstract]

2024 Apr:126:155200. PMID: 38387273
Biochem Pharmacol

Interplay between G protein-biased and arrestin-biased pathways in 5-HT2AR-mediated ERK activation. [Abstract]

2025 Sep:239:117015. PMID: 40473228

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (125.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.2577 mL

6.2884 mL

12.5769 mL

5 mM

0.2515 mL

1.2577 mL

2.5154 mL

10 mM

0.1258 mL

0.6288 mL

1.2577 mL

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

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体内:

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

Stock Solution Working Solution

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 (3.14 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (3.14 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (3.14 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:

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mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
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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).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (281 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Favre-Guilmard C, et al. The novel inhibitor of the heterotrimeric G-protein complex, BIM-46187, elicits anti-hyperalgesic properties and synergizes with morphine. Eur J Pharmacol. 2008 Oct 10;594(1-3):70-6. [Content Brief]

[2]. Dela Paz NG, et al. Rapid flow-induced activation of Gαq/11 is independent of Piezo1 activation. Am J Physiol Cell Physiol. 2019 May 1;316(5):C741-C752. [Content Brief]

[3]. Haase J, et al. Sex and brain region-specific regulation of serotonin transporter activity in synaptosomes in guanine nucleotide-binding protein G(q) alpha knockout mice. J Neurochem. 2021 Oct;159(1):156-171. [Content Brief]

[4]. Auguet M, et al. SYNERGISTIC ANALGESIC INTERACTION BETWEEN MORPHINE AND BIM‐46187. European Journal of Pain, 2006, 10(S1): S89-S89.

[5]. Silvente-Poirot S, et al. Heterotrimeric G-protein inhibitor BIM-46187 inhibits G-protein coupled receptor dependent tumorigenesis in athymic mice. Cancer Research, 2007, 67(9_Supplement): 5603-5603.

[6]. Joshi JC, et al. RGS2 is an innate immune checkpoint for suppressing Gαq-mediated IFNγ generation and lung injury. iScience. 2025 Jan 27;28(2):111878. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.2577 mL	6.2884 mL	12.5769 mL	31.4422 mL
	5 mM	0.2515 mL	1.2577 mL	2.5154 mL	6.2884 mL
	10 mM	0.1258 mL	0.6288 mL	1.2577 mL	3.1442 mL
	15 mM	0.0838 mL	0.4192 mL	0.8385 mL	2.0961 mL
	20 mM	0.0629 mL	0.3144 mL	0.6288 mL	1.5721 mL
	25 mM	0.0503 mL	0.2515 mL	0.5031 mL	1.2577 mL
	30 mM	0.0419 mL	0.2096 mL	0.4192 mL	1.0481 mL
	40 mM	0.0314 mL	0.1572 mL	0.3144 mL	0.7861 mL
	50 mM	0.0252 mL	0.1258 mL	0.2515 mL	0.6288 mL
	60 mM	0.0210 mL	0.1048 mL	0.2096 mL	0.5240 mL
	80 mM	0.0157 mL	0.0786 mL	0.1572 mL	0.3930 mL
	100 mM	0.0126 mL	0.0629 mL	0.1258 mL	0.3144 mL

Keywords

PH-064

2 Cited Publications

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PH-064

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MedChemExpress（MCE）の使用を引用している文献 PH-064

Akt アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (2)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

PH-064 関連分類

HY-10499 関連分類