country

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-12850

Copy Link Print Information

Dasotraline

(Synonyms: SEP 225289)

Dasotraline is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC₅₀ values of 4, 6, and 11 nM, respectively.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No.: 675126-05-3
화학식: C₁₆H₁₅Cl₂N
분자량:292.20

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

Dasotraline Chemical Structure

CAS No.: 675126-05-3

사이즈

가격

재고

수량

Sample (0.1mg)

In-stock

(In Japan)

Apply Now

견적 받기 Ask For Quote & Lead Time Consult sales personnel for more information Check price and availability 견적 받기 Ask For Quote & Lead Time Consult sales personnel for more information Check price and availability

대량구매 문의

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vivo
- Clinical Trial
Chemical Information
용액&용해도
- In Vitro
순도&문서
References
Help & FAQs
Bioz

Biological Activity

제품 설명

Dasotraline is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC₅₀ values of 4, 6, and 11 nM, respectively.

IC₅₀ & Target

IC50: 4 nM (dopamine transporter), 6 nM (norepinephrine transporter),11 nM (5-HT transporter)^[1]

In Vivo

The present in-vivoelectrophysiological study is undertaken to determine the effects of the triple reuptake inhibitor Dasotraline (SEP-225289) on the neuronal activities of locus coeruleus (LC) NE, ventral tegmental area (VTA) DA and dorsal raphe (DR) 5-HT neurons. Administered acutely, Dasotraline dose-dependently decreases the spontaneous firing rate of LC NE, VTA DA and DR 5-HT neurons through the activation of α₂, D₂ and 5-HT_1A autoreceptors, respectively. Dasotraline predominantly inhibits the firing rate of LC NE neurons while producing only a partial decrease in VTA DA and DR 5-HT neuronal discharge. Dasotraline is equipotent at inhibiting 5-HT and NE transporters since it prolongs to the same extent the time required for a 50% recovery (RT₅₀) of the firing activity of dorsal hippocampus CA3 pyramidal neurons from the inhibition induced by microiontophoretic application of 5-HT and NE. The recovery time (RT), from the suppression of hippocampus pyramidal neuron firing activity following microiontophoresis application of 5-HT and NE, is assessed by determining the RT₅₀ values before and after the acute intravenous administration of cumulative doses of Dasotraline (1–8 mg/kg). Although Dasotraline (1 and 2 mg/kg) does not modify the firing activity of CA3 pyramidal neurons, a significant reduction (∼50%) is detected with the highest dose (8 mg/kg). In rats pre-treated with WAY100635, Dasotraline (0.5-2 mg/kg i.v.) elicits a significant increase in DR 5-HT firing rate. In rats pre-treated with WAY100635, Dasotralinesignificantly increases the number of single spikes and bursts^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 675126-05-3
분자량 292.20
화학식 C₁₆H₁₅Cl₂N
SMILES

N[C@@H]1CC[C@@H](C2=CC=C(Cl)C(Cl)=C2)C3=CC=CC=C31
Synonyms

SEP 225289
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

용액&용해도

In Vitro:

DMSO : ≥ 31 mg/mL (106.09 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

3.4223 mL

17.1116 mL

34.2231 mL

5 mM

0.6845 mL

3.4223 mL

6.8446 mL

10 mM

0.3422 mL

1.7112 mL

3.4223 mL

몰농도 계산기

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

Mass

Concentration

Volume

Molecular Weight

농도 희석 계산기

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.

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

Working solution concentration: 0.22 mg/mL

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (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)
Handling Instructions (2659 KB)

References

[1]. Guiard BP, et al. Characterization of the electrophysiological properties of triple reuptake inhibitors on monoaminergic neurons. Int J Neuropsychopharmacol. 2011 Mar;14(2):211-23. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.4223 mL	17.1116 mL	34.2231 mL	85.5578 mL
	5 mM	0.6845 mL	3.4223 mL	6.8446 mL	17.1116 mL
	10 mM	0.3422 mL	1.7112 mL	3.4223 mL	8.5558 mL
	15 mM	0.2282 mL	1.1408 mL	2.2815 mL	5.7039 mL
	20 mM	0.1711 mL	0.8556 mL	1.7112 mL	4.2779 mL
	25 mM	0.1369 mL	0.6845 mL	1.3689 mL	3.4223 mL
	30 mM	0.1141 mL	0.5704 mL	1.1408 mL	2.8519 mL
	40 mM	0.0856 mL	0.4278 mL	0.8556 mL	2.1389 mL
	50 mM	0.0684 mL	0.3422 mL	0.6845 mL	1.7112 mL
	60 mM	0.0570 mL	0.2852 mL	0.5704 mL	1.4260 mL
	80 mM	0.0428 mL	0.2139 mL	0.4278 mL	1.0695 mL
	100 mM	0.0342 mL	0.1711 mL	0.3422 mL	0.8556 mL

Keywords

100 mg

견적 받기 해외재고보유

Price: USD 0.00

Biological Activity
- 제품 설명
- IC50 & Target
- In Vivo
- Clinical Trial
Chemical Information
용액&용해도
- In Vitro
- In Vivo Dissolution Calculator
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

Dasotraline

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

Dasotraline Related Classifications

Cat. No.: HY-12850