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VU0152100

Alias: VU-152100VU-0152100VU 0152100VU0152100VU152100VU 152100
Cat No.:V7519 Purity: ≥98%
VU0152100 (VU152100) is a selective positive allosteric modulator (PAM) of mAChR (BBB (blood-brain barrier) permeable/penetrable).
VU0152100
VU0152100 Chemical Structure CAS No.: 409351-28-6
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
VU0152100 (VU152100) is a selective positive allosteric modulator (PAM) of mAChR (BBB (blood-brain barrier) permeable/penetrable). VU0152100 reverses amphetamine-induced hyperlocomotion and increased extracellular dopamine levels in the nucleus accumbens and caudate-putamen in rats. VU0152100 has good research potential in psychosis and cognitive impairment related to mental disorders (like schizophrenia).
Biological Activity I Assay Protocols (From Reference)
ln Vivo
VU0152100 (10, 30, 56.6 mg/kg; ip; single) counteracts hypermotility brought on by amphetamines [1]. VU0152100 (10, 30, 56.6 mg/kg; ip; single) counteracts hypermotility brought on by amphetamines [1]. In the nucleus accumbens and caudate-putamen, VU0152100 reverses amphetamine-induced elevations in extracellular dopamine levels [1].
Animal Protocol
Animal/Disease Models: Adult male SD (SD (Sprague-Dawley)) rat (250-275 g; amphetamine-induced hyperlocomotion model) [1].
Doses: 10, 30, 56.6 mg/kg
Route of Administration: intraperitoneal (ip) injection; Single (pre-treatment)
Experimental Results: Powerful dose-dependent reversal of amphetamine-induced hyperkinesis.

Animal/Disease Models: Adult male SD (SD (Sprague-Dawley)) rat (250-275 g; amphetamine induction) [1].
Doses: 10, 30, 56.6 mg/kg
Route of Administration: intraperitoneal (ip) injection; Single (pre-treatment)
Experimental Results: Blocked amphetamine-induced disruption of prepulse inhibition. Dose-dependently reversed the disruptive effects of amphetamine on the acquisition of context-dependent fear.
References

[1]. Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100. Neuropsychopharmacology. 2014 Jun;39(7):1578-93.

[2]. Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats. J Pharmacol Exp Ther. 2008 Dec;327(3):941-53.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H19N3O2S
Molecular Weight
341.429
Exact Mass
341.12
CAS #
409351-28-6
PubChem CID
864492
Appearance
Light yellow to khaki solid powder
LogP
4.406
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
5
Rotatable Bond Count
4
Heavy Atom Count
24
Complexity
442
Defined Atom Stereocenter Count
0
InChi Key
MDNWGCQSCGNTKH-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H19N3O2S/c1-10-8-11(2)21-18-14(10)15(19)16(24-18)17(22)20-9-12-4-6-13(23-3)7-5-12/h4-8H,9,19H2,1-3H3,(H,20,22)
Chemical Name
3-amino-N-[(4-methoxyphenyl)methyl]-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide
Synonyms
VU-152100VU-0152100VU 0152100VU0152100VU152100VU 152100
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ≥ 50 mg/mL (~146.44 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (7.32 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.9289 mL 14.6443 mL 29.2886 mL
5 mM 0.5858 mL 2.9289 mL 5.8577 mL
10 mM 0.2929 mL 1.4644 mL 2.9289 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • VU0152100 reverses amphetamine-induced hyperlocomotion in rats and wild-type mice, but not in M4 KO mice. (a) Amphetamine-induced (1 mg/kg) hyperlocomotion in rats is dose-dependently reversed by VU0152100 (*p<0.05 vs vehicle/amphetamine (Dunnett's test)); (b) VU0152100 reverses amphetamine-induced hyperlocomotion in wild-type mice. (c) In M4 KO mice, amphetamine-induced hyperlocomotion is not blocked by VU0152100 (*p<0.05, vehicle/amphetamine (Bonferroni's test)). Data are mean±SEM of 8 rats or 10–11 mice per group.[1].Byun NE, et al. Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100. Neuropsychopharmacology. 2014 Jun;39(7):1578-93.
  • VU0152100 reverses sensorimotor gating and contextual fear conditioning deficits elicited by amphetamine. (a) VU0152100 blocks amphetamine-induced (3 mg/kg) disruption of prepulse inhibition (*p<0.05 vs vehicle/vehicle (Dunnett's test)); (b) The disruptive effects of amphetamine (4.8 mg/kg, s.c.) on the acquisition of a context-dependent fear response are dose-dependently reversed by pre-treatment with VU0152100 (**p<0.01, ***p<0.001 vs vehicle/vehicle, #p<0.05 vs vehicle/amphetamine (Dunnett's test)). Data are mean±SEM of 7–11 rats per group.[1].Byun NE, et al. Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100. Neuropsychopharmacology. 2014 Jun;39(7):1578-93.
  • VU0152100 modulates amphetamine-induced cerebral blood volume (CBV) responses. (a) Amphetamine (1 mg/kg, i.p.) elicited CBV increases, reflecting neural activity, while pre-treatment with VU0152100 (56.6 mg/g, i.p.) suppressed this effect in multiple brain areas. (b) Regional CBV time courses for amphetamine and reversal by VU0152100 are shown for the retrosplenial cortex, medial thalamus, hippocampus, NAS, CP, and PFC; note that amphetamine by itself and in combination with VU0152100 did not alter CBV in the PFC. Data are means±SEM of 10–11 animals per group. Functional connectivity analysis of the phMRI data revealed fewer inter-regional correlations in the VU0152100/amphetamine group and the significant ROI–ROI correlation differences between the vehicle/amphetamine group and the VU0152100/amphetamine group (thresholded at p<0.05) are depicted in panel (c). Cells are colored according to the corresponding z-statistic. Abbreviations of regions of interest (number indicates slice): Amyg, amygdala; CP, caudate-putamen; Cg, cingulate; Hipp, hippocampus; MT, medial thalamus; M, motor cortex; NAS, nucleus accumbens; PFC, prefrontal cortex; Pir, piriform cortex; Rs, retrosplenial cortex; S, sensory cortex; SN, substantia nigra; V, visual cortex.[1].Byun NE, et al. Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100. Neuropsychopharmacology. 2014 Jun;39(7):1578-93.
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