Taltirelin acetate (Synonyms: TA-0910 acetate)

Name: Taltirelin acetate
Brand: MedChemExpress
SKU: HY-B0596A
Rating: 4.5 (1 reviews)

Cat. No.: HY-B0596A Purity: 98.77%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Taltirelin acetate (TA-0910) is an acetate form of Taltirelin (TA-0910). Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC₅₀ at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca²⁺ concentration (Ca²⁺ release) with an EC₅₀ value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue.

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Taltirelin acetate Chemical Structure

CAS No. : 1549593-23-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 96	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 310	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 496	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of Taltirelin acetate:

Taltirelin In-stock
Taltirelin-¹³C,d₃ Get quote

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Description

IC₅₀ & Target

IC₅₀: 910 nM (Thyrotropin-releasing hormone receptor)^[1]

In Vitro

Taltirelin (5 μM; 2 h) improves cell viability, reducess ROS production and apoptosis in MPP+ (HY-W008719) or Rotenone (HY-B1756) treated SH-SY5Y cells and primary rat midbrain neurons^[2].
Taltirelin (5 μM; 2 h) exerts neuroprotective effects by inhibiting tau phosphorylation and AEP activation in SH-SY5Y cells treated with MPP+ (HY-W008719) or rotenone (HY-B1756)^[2].

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

Cell Viability Assay^[2]

Cell Line:	SH-SY5Y neuroblastoma cells and primary neonatal rat midbrain neurons
Concentration:	5 μM
Incubation Time:	2 h
Result:	Increased cell viability.

Western Blot Analysis^[2]

Cell Line:	SH-SY5Y neuroblastoma cells
Concentration:	5 μM
Incubation Time:	2 h
Result:	Prevented the elevation of the cleaved caspase-3.

Cell Viability Assay^[2]

Cell Line:	SH-SY5Y neuroblastoma cells
Concentration:	5 μM
Incubation Time:	2 h
Result:	Reduced the levels of p-tau and AEP cleavage products: tau N368 and a-synuclein N103 fragments.

In Vivo

Dosage of Taltirelin in non-salt form:
Taltirelin (0.2-5 mg/kg; Intraperitoneal injection; 14-56 days) has a neuroprotective effect in mouse models of MPTP (HY-15608) and chronic rotenone (HY-B1756) -induced PD, and improves locomotor function in mice ^[2].
Taltirelin (1 mg/kg Intraperitoneal injection; 10 mg/kg Oral administration; 1 day) alleviates the fatigue-like behavior caused by chemotherapy treatment, tumor burden and irradiation in mouse models ^[3].

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

Animal Model:	MPTP (HY-15608) or Rotenone (HY-B1756) treated male C57/BL6 mice aged 8-9 weeks old^[2]
Dosage:	0.2 mg/kg, 1 mg/kg, 5 mg/kg 14 days; 0.2 mg/kg, 1 mg/kg 56 days
Administration:	Intraperitoneal injection (i.p.)
Result:	Improved the locomotor function and preserved dopaminergic neurons in the substantia nigra. Down-regulated the levels of p-tau (S396), p-α-synuclein (S129) tau N368 and α-synuclein N103 fragments in substantia nigra and striatum.

Animal Model:	5-FU (HY-90006) or radiation treated adult C57BL/6NCr mice aged 7-8 weeks; Balb/cAnNCr mice aged 9 weeks old with colon 26 carcinoma^[3]
Dosage:	1mg/kg; 10mg/kg
Administration:	Intraperitoneal injection (i.p.); Oral administration (p.o.); Twice a day before the test and once again 30 minutes prior to the test.
Result:	Reversed the fatigue-like effect, caused mice to run nearer to the top of the treadmill during the test.

Molecular Weight

465.46

Formula

C₁₉H₂₇N₇O₇

CAS No.

1549593-23-8

Appearance

Solid

Color

White to off-white

SMILES

O=C(N(CCC1)[C@@H]1C(N)=O)[C@@H](NC([C@@H](NC2=O)CC(N2C)=O)=O)CC3=CN=CN3.CC(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (268.55 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	2.1484 mL	10.7421 mL	21.4841 mL
5 mM	0.4297 mL	2.1484 mL	4.2968 mL
10 mM	0.2148 mL	1.0742 mL	2.1484 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 (sealed storage, away from moisture). 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)

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: ≥ 2.08 mg/mL (4.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 98.77%

Select Batch:

Data Sheet (283 KB) SDS (252 KB)

COA (255 KB) RP-HPLC (206 KB) MS (179 KB)

Handling Instructions (2659 KB)

References

[1]. Thirunarayanan N, et al. Taltirelin is a superagonist at the human thyrotropin-releasing hormone receptor. Front Endocrinol (Lausanne). 2012 Oct 9;3:120. [Content Brief]

[2]. Zheng C, et al. TRH Analog, Taltirelin Protects Dopaminergic Neurons From Neurotoxicity of MPTP and Rotenone. Front Cell Neurosci. 2018 Dec 20;12:485. [Content Brief]

[3]. Dougherty JP, et al. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue. Pharmacol Res. 2017 Oct;124:1-8. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.1484 mL	10.7421 mL	21.4841 mL	53.7103 mL
	5 mM	0.4297 mL	2.1484 mL	4.2968 mL	10.7421 mL
	10 mM	0.2148 mL	1.0742 mL	2.1484 mL	5.3710 mL
	15 mM	0.1432 mL	0.7161 mL	1.4323 mL	3.5807 mL
	20 mM	0.1074 mL	0.5371 mL	1.0742 mL	2.6855 mL
	25 mM	0.0859 mL	0.4297 mL	0.8594 mL	2.1484 mL
	30 mM	0.0716 mL	0.3581 mL	0.7161 mL	1.7903 mL
	40 mM	0.0537 mL	0.2686 mL	0.5371 mL	1.3428 mL
	50 mM	0.0430 mL	0.2148 mL	0.4297 mL	1.0742 mL
	60 mM	0.0358 mL	0.1790 mL	0.3581 mL	0.8952 mL
	80 mM	0.0269 mL	0.1343 mL	0.2686 mL	0.6714 mL
	100 mM	0.0215 mL	0.1074 mL	0.2148 mL	0.5371 mL

Taltirelin acetate Related Classifications

Neurological Disease Endocrinology

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:

Taltirelin1549593-23-8TA-0910TA0910TA 0910Thyroid Hormone ReceptorApoptosisTHRTRHSH-SY5Y cellsPrimary rat mesencephalic neuronsCa²⁺PDInhibitorinhibitorinhibit

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Taltirelin acetate (Synonyms: TA-0910 acetate)

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Complete Stock Solution Preparation Table

Taltirelin acetate Related Classifications

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