2. GPCR/G Protein
  3. PTHR
  4. PCO371

PCO371 is an orally active full agonist of parathyroid hormone receptor 1 (PTHR1), with no effect on PTH type 2 receptor.

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PCO371

PCO371 Chemische Struktur

CAS. Nr. : 1613373-33-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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Other Forms of PCO371:

PCO371 Related Antibodies

Top Publications Citing Use of Products

Alle PTHR Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
PTH1R PTH2R

  • Biologische Aktivität

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Beschreibung

PCO371 is an orally active full agonist of parathyroid hormone receptor 1 (PTHR1), with no effect on PTH type 2 receptor.

IC50 & Target

PTHR1[1]
Cellular Effect
Cell Line Type Value Description References
LLC-PK1 EC50
4.1 3
Compound: 16c; PCO371
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
[PMID: 32022560]
LLC-PK1 EC50
4.1 3
Compound: 16c; PCO371
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
[PMID: 32022560]
LLC-PK1 EC50
4.1 3
Compound: 16c; PCO371
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
Agonist activity at recombinant human PTHR1 expressed in pig LLC-PK1 cells assessed as increase in cAMP production measured after 20 mins by EIA
[PMID: 32022560]
In Vitro

PCO371 is an orally active full agonist of parathyroid hormone receptor 1 (PTHR1), with no effect on PTH type 2 receptor. PCO371 induces cAMP production with an EC50 of 2.4 μM in COS-7 cells expressing hPTHR1, and 2.5 μM in COS-7 cells transfected with hPTHR1-delNT, and also enhances the phospholipase C activity (EC50, 17 μM)[1].

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

PCO371 Related Antibodies
Klinische Studie
Molekulargewicht

635.65

Formel

C29H32F3N5O6S
CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

FC(F)(F)OC1=CC=C(C2=NC3(CCN(S(CCC4=C(C)C=C(N5C(NC(C5(C)C)=O)=O)C=C4C)(=O)=O)CC3)C(N2)=O)C=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 100 mg/mL (157.32 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 1.5732 mL 7.8660 mL 15.7319 mL
5 mM 0.3146 mL 1.5732 mL 3.1464 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.

  • Molaritätsrechner

  • Verdünnungsrechner

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 (3.93 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 (3.93 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.
Reinheit & Dokumentation

Purity: 99.67%

SDS (393 KB)

COA (247 KB) HNMR (319 KB) CNMR (306 KB) RP-HPLC (255 KB) LCMS (109 KB)

Handling Instructions (2659 KB)
Verweise

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 1.5732 mL 7.8660 mL 15.7319 mL 39.3298 mL
5 mM 0.3146 mL 1.5732 mL 3.1464 mL 7.8660 mL
10 mM 0.1573 mL 0.7866 mL 1.5732 mL 3.9330 mL
15 mM 0.1049 mL 0.5244 mL 1.0488 mL 2.6220 mL
20 mM 0.0787 mL 0.3933 mL 0.7866 mL 1.9665 mL
25 mM 0.0629 mL 0.3146 mL 0.6293 mL 1.5732 mL
30 mM 0.0524 mL 0.2622 mL 0.5244 mL 1.3110 mL
40 mM 0.0393 mL 0.1966 mL 0.3933 mL 0.9832 mL
50 mM 0.0315 mL 0.1573 mL 0.3146 mL 0.7866 mL
60 mM 0.0262 mL 0.1311 mL 0.2622 mL 0.6555 mL
80 mM 0.0197 mL 0.0983 mL 0.1966 mL 0.4916 mL
100 mM 0.0157 mL 0.0787 mL 0.1573 mL 0.3933 mL
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PCO371 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:

PCO3711613373-33-3PCO 371PCO-371PTHRParathyroid hormone receptorInhibitorinhibitorinhibit

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SAFETY DATA SHEET (SDS)

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