2. GPCR/G Protein
  3. Oxytocin Receptor
  4. LIT-001 free base

LIT-001 free base is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM). LIT-001 free base improves social interaction in a mouse model of autism.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (LIT-001) usually boasts enhanced water solubility and stability.

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

LIT-001 free base

LIT-001 free base Chemical Structure

CAS No. : 2245072-20-0

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Other Forms of LIT-001 free base:

LIT-001 free base Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

LIT-001 free base is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM). LIT-001 free base improves social interaction in a mouse model of autism[1].

In Vitro

In vitro signaling experiments, LIT-001 free base is a nonbiased OT-R agonist on the two main signaling pathways of this receptor, with minor antagonist effect on V1a and agonist effect on V1b receptors, observed at high concentrations only[1].

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

LIT-001 free base Related Antibodies
In Vivo

LIT-001 free base (10-20 mg/kg; i.p.) alleviates core symptoms in the context of autism spectrum disorders (ASD )[1].

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

Animal Model: Oprm1–/– mice (bred in house on a 50% 129SVPas–50% C57BL/6J hybrid background)[1]
Dosage: 10, 20 mg/kg
Administration: i.p.
Result: Alleviated core symptoms in the context of ASD.
Molecular Weight

531.67

Formula

C28H33N7O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1[C@H](C(N(C)C)=S)CCC1)NCC2=CC=C(C(N3CC4=C(N(C)N=C4)NC5=CC=CC=C35)=O)C=C2C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (188.09 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 1.8809 mL 9.4043 mL 18.8087 mL
5 mM 0.3762 mL 1.8809 mL 3.7617 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. 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)

Mass
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Concentration
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Volume
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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 (4.70 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 (4.70 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.
Purity & Documentation
References

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8809 mL 9.4043 mL 18.8087 mL 47.0217 mL
5 mM 0.3762 mL 1.8809 mL 3.7617 mL 9.4043 mL
10 mM 0.1881 mL 0.9404 mL 1.8809 mL 4.7022 mL
15 mM 0.1254 mL 0.6270 mL 1.2539 mL 3.1348 mL
20 mM 0.0940 mL 0.4702 mL 0.9404 mL 2.3511 mL
25 mM 0.0752 mL 0.3762 mL 0.7523 mL 1.8809 mL
30 mM 0.0627 mL 0.3135 mL 0.6270 mL 1.5674 mL
40 mM 0.0470 mL 0.2351 mL 0.4702 mL 1.1755 mL
50 mM 0.0376 mL 0.1881 mL 0.3762 mL 0.9404 mL
60 mM 0.0313 mL 0.1567 mL 0.3135 mL 0.7837 mL
80 mM 0.0235 mL 0.1176 mL 0.2351 mL 0.5878 mL
100 mM 0.0188 mL 0.0940 mL 0.1881 mL 0.4702 mL
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LIT-001 free base 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:

LIT-0012245072-20-0LIT001LIT 001Oxytocin ReceptorOXTRnonpeptidesocialinteractionV1aV2vasopressinreceptorautismspectrumdisordersnonbiasedInhibitorinhibitorinhibit

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