2. Neuronal Signaling PI3K/Akt/mTOR
  3. Serotonin Transporter Akt
  4. PH-064

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.

For research use only. We do not sell to patients.

PH-064

PH-064 Chemical Structure

CAS No. : 892546-37-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of PH-064:

PH-064 Related Antibodies

Top Publications Citing Use of Products

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3][4][5][6].

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]
In Vitro

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.

PH-064 Related Antibodies
In Vivo

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).
Molecular Weight

795.11

Formula

C44H58N8O2S2
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2577 mL 6.2884 mL 12.5769 mL
5 mM 0.2515 mL 1.2577 mL 2.5154 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, 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.

  • 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)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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 (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.

    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% (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.

    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.
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.
Purity & Documentation

Purity: 99.88%

SDS (393 KB)

COA (251 KB) HNMR (326 KB) LCMS (265 KB)

Handling Instructions (2659 KB)
References

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, 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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PH-064 Related Classifications

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:

PH-064892546-37-1BIM-46187PH064PH 064BIM46187BIM 46187Serotonin TransporterAkt5-HTTSERTSLC6A4PKBProtein kinase BInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PH-064
Cat. No.:
HY-10499
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB) Italian - IT (393 KB) Korean - KR (393 KB) Portuguese - PT (393 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.