LY3154207

Cat. No.: HY-128770 Purity: 99.87%: FAQs
Data Sheet SDS COA Handling Instructions

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LY3154207 is a potent, subtype selective, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC₅₀=3 nM).

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

LY3154207 Chemical Structure

CAS No. : 1638667-79-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 528	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 528	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 800	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2250	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3250	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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

Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE LY3154207

•Nat Commun. 2022 Jun 8;13(1):3186. [Abstract]

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Dopamine Receptor D₁ Receptor D₂ Receptor D₃ Receptor D₄ Receptor D₅ Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

LY3154207 is a potent, subtype selective, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC₅₀=3 nM)^[1].

IC₅₀ & Target

EC50: 3 nM (human dopamine D1 receptor)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	> 10000 nM Compound: 3; LY3154207	Positive allosteric modulator activity at human D5 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay Positive allosteric modulator activity at human D5 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay	[PMID: 31532644]
HEK293	EC₅₀	1.11 nM Compound: 35; LY3154207	Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay Positive allosteric modulation of human D1R expressed in HEK293 cells assessed as increase in dopamine-induced cAMP accumulation after 60 mins by HTRF assay	[PMID: 30525590]
HEK293	EC₅₀	12.8 nM Compound: 3; LY3154207	Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 60 mins by HTRF assay Agonist activity at human D1 receptor stably expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 60 mins by HTRF assay	[PMID: 31532644]
HEK293	EC₅₀	2 nM Compound: 3; LY3154207	Positive allosteric modulator activity at dog D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay Positive allosteric modulator activity at dog D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay	[PMID: 31532644]
HEK293	EC₅₀	2.3 nM Compound: 3; LY3154207	Positive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay Positive allosteric modulator activity at human D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay	[PMID: 31532644]
HEK293	EC₅₀	2.5 nM Compound: 3; LY3154207	Positive allosteric modulator activity at rhesus monkey D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay Positive allosteric modulator activity at rhesus monkey D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay	[PMID: 31532644]
HEK293	EC₅₀	3 nM Compound: 3; LY3154207	Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay Positive allosteric modulator activity at human D1 receptor stably expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay	[PMID: 31532644]
HEK293	EC₅₀	62.1 nM Compound: 3; LY3154207	Positive allosteric modulator activity at mouse D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay Positive allosteric modulator activity at mouse D1 receptor transiently expressed in HEK293 cells assessed as potentiation of EC20 dopamine-induced cAMP accumulation incubated for 60 mins by HTRF assay	[PMID: 31532644]

In Vitro

In HEK293 cells transiently expressing human, dog, rhesus monkey, and mouse D1 receptors, the EC₅₀s of LY3154207 are 2.3 nM, 2.0 nM, 2.5 nM, and 62.1 nM, respectively^[1].

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

Clinical Trial

Molecular Weight

450.40

Formula

C₂₄H₂₉Cl₂NO₃

CAS No.

1638667-79-4

Appearance

Solid

Color

White to off-white

SMILES

O=C(N1[C@@H](C)C2=C(C(CCC(C)(O)C)=CC=C2)C[C@@H]1CO)CC3=C(Cl)C=CC=C3Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 110 mg/mL (244.23 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	2.2202 mL	11.1012 mL	22.2025 mL
5 mM	0.4440 mL	2.2202 mL	4.4405 mL
10 mM	0.2220 mL	1.1101 mL	2.2202 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)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 2.75 mg/mL (6.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (6.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.75 mg/mL (6.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 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 (27.5 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)

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: 99.87%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (253 KB) LCMS (86 KB)

Handling Instructions (2659 KB)

References

[1]. Hao J, Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1S,3R)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Po [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2202 mL	11.1012 mL	22.2025 mL	55.5062 mL
	5 mM	0.4440 mL	2.2202 mL	4.4405 mL	11.1012 mL
	10 mM	0.2220 mL	1.1101 mL	2.2202 mL	5.5506 mL
	15 mM	0.1480 mL	0.7401 mL	1.4802 mL	3.7004 mL
	20 mM	0.1110 mL	0.5551 mL	1.1101 mL	2.7753 mL
	25 mM	0.0888 mL	0.4440 mL	0.8881 mL	2.2202 mL
	30 mM	0.0740 mL	0.3700 mL	0.7401 mL	1.8502 mL
	40 mM	0.0555 mL	0.2775 mL	0.5551 mL	1.3877 mL
	50 mM	0.0444 mL	0.2220 mL	0.4440 mL	1.1101 mL
	60 mM	0.0370 mL	0.1850 mL	0.3700 mL	0.9251 mL
	80 mM	0.0278 mL	0.1388 mL	0.2775 mL	0.6938 mL
	100 mM	0.0222 mL	0.1110 mL	0.2220 mL	0.5551 mL

LY3154207 Related Classifications

Neurological Disease

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:

LY31542071638667-79-4LY 3154207LY-3154207Dopamine ReceptorInhibitorinhibitorinhibit

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LY3154207

Customer Review

LY3154207 Related Antibodies

1 Publications Citing Use of MCE LY3154207

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•Related Screening Libraries:

•Related Small Molecules:

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View All Dopamine Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

LY3154207 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

LY3154207 Related Classifications

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Customer Review

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