[CAS NO. 1643462-64-9] (Rac)-Tavapadon

Name: (Rac)-Tavapadon
Brand: Arctom Scientific
SKU: AS945306

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PRODUCTS SPECIFICATIONS [1643462-64-9]

Distributor

Catalog

AS945306

Brand

Arctom Scientific

CAS

1643462-64-9

DESCRIPTION [1643462-64-9]

Overview

MDL	MFCD32669809
Molecular Weight	391.34
Molecular Formula	C19H16F3N3O3
SMILES	O=C1NC(C(C)=C(C2=CC=C(OC3=NC=CC=C3C(F)(F)F)C=C2C)N1C)=O

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

Summary

(Rac)-Tavapadon ((Rac)-PF-06649751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC ₅₀ =0.8 nM; β-arrestin2, EC ₅₀ =68 nM). (Rac)-Tavapadon has antiparkinsonian activity ^[1] .

IC50 & Target

D ₁ Receptor

In Vitro

(Rac)-Tavapadon ((Rac)-PF-06649751; compound 32) has E _MAX s of 118% and 30% in the GS activation assay and the β-arrestin2 recruitment assay ^[1] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02066909	Pfizer	Healthy	February 2014	Phase 1
NCT02373072	Pfizer	Idiopathic Parkinson Disease	March 2015	Phase 1
NCT02262767	Pfizer	Healthy	November 2014	Phase 1
NCT04201093	Cerevel Therapeutics, LLC	Parkinson Disease	December 13, 2019	Phase 3
NCT05404529	Cerevel Therapeutics, LLC	Hepatic Impairment	April 29, 2022	Phase 1
NCT05581823	Cerevel Therapeutics, LLC	Parkinson Disease	October 19, 2022	Phase 1
NCT04760769	Cerevel Therapeutics, LLC	Parkinson Disease	February 24, 2021	Phase 3
NCT05404542	Cerevel Therapeutics, LLC	Renal Impairment	May 10, 2022	Phase 1
NCT04223193	Cerevel Therapeutics, LLC	Parkinson Disease	January 6, 2020	Phase 3
NCT04241393	Cerevel Therapeutics, LLC	Healthy Subjects	February 4, 2020	Phase 1
NCT04295642	Cerevel Therapeutics, LLC	Parkinson Disease	January 8, 2020	Phase 1
NCT03185481	Pfizer	Parkinson´s Disease With Motor Fluctuations	July 6, 2017	Phase 2
NCT02847650	Pfizer	Parkinson Disease	October 17, 2016	Phase 2
NCT02687542	Pfizer	Parkinson Disease	March 3, 2016	Phase 2
NCT02224664	Pfizer	Parkinson´s Disease	October 2014	Phase 1
NCT05610189	Cerevel Therapeutics, LLC	Parkinson Disease	December 13, 2022	Phase 1
NCT04542499	Cerevel Therapeutics, LLC	Parkinson Disease	October 27, 2020	Phase 3
NCT01981694	Pfizer	Healthy	November 2013	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 41.67 mg/mL ( 106.48 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5553 mL	12.7766 mL	25.5532 mL
5 mM	0.5111 mL	2.5553 mL	5.1106 mL
10 mM	0.2555 mL	1.2777 mL	2.5553 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 4.17 mg/mL (10.66 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Michael L Martini, et al. Designing Functionally Selective Noncatechol Dopamine D 1 Receptor Agonists with Potent In Vivo Antiparkinsonian Activity. ACS Chem Neurosci. 2019 Sep 18;10(9):4160-4182.