PBD-150

Name: PBD-150
Brand: MedChemExpress
SKU: HY-119173
Rating: 4.5 (1 reviews)

Cat. No.: HY-119173 Purity: 98.39%: FAQs
Data Sheet SDS COA Handling Instructions

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PBD-150 is a human glutaminyl cyclase (hQC) Y115E-Y117E variant inhibitor, with a K_i value of 490 nM.

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

PBD-150 Chemical Structure

CAS No. : 790663-33-1

Size	Price	Stock	Quantity
5 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 112	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 224	In-stock	Estimated Time of Arrival: December 31
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100 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Description

PBD-150 is a human glutaminyl cyclase (hQC) Y115E-Y117E variant inhibitor, with a K_i value of 490 nM^[1]^[2].

In Vivo

PBD-150 is able to reduce the deposition of pyroglutamate-modified amyloid-β peptides in brain of transgenic mouse models of Alzheimer disease, leading to a significant improvement of learning and memory in those transgenic animals^[3].

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

Molecular Weight

320.41

Formula

C₁₅H₂₀N₄O₂S

CAS No.

790663-33-1

Appearance

Solid

Color

Light brown to brown

SMILES

S=C(NCCCN1C=CN=C1)NC2=CC=C(OC)C(OC)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (390.13 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	3.1210 mL	15.6050 mL	31.2100 mL
5 mM	0.6242 mL	3.1210 mL	6.2420 mL
10 mM	0.3121 mL	1.5605 mL	3.1210 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)

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 (6.49 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 (6.49 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 (6.49 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).

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: 98.39%

Select Batch:

Data Sheet (271 KB) SDS (393 KB)

COA (244 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[1]. Buchholz M, et al. The first potent inhibitors for human glutaminyl cyclase: synthesis and structure-activity relationship. J Med Chem. 2006 Jan 26;49(2):664-77. [Content Brief]

[2]. DiPisa F, et al. The soluble Y115E-Y117E variant of human glutaminyl cyclase is a valid target for X-ray and NMR screening of inhibitors against Alzheimer disease. Acta Crystallogr F Struct Biol Commun. 2015 Aug;71(Pt 8):986-92. [Content Brief]

[3]. Huang KF, et al. Structures of human Golgi-resident glutaminyl cyclase and its complexes with inhibitors reveal a large loop movement upon inhibitor binding. J Biol Chem. 2011 Apr 8;286(14):12439-49. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	3.1210 mL	15.6050 mL	31.2100 mL	78.0250 mL
	5 mM	0.6242 mL	3.1210 mL	6.2420 mL	15.6050 mL
	10 mM	0.3121 mL	1.5605 mL	3.1210 mL	7.8025 mL
	15 mM	0.2081 mL	1.0403 mL	2.0807 mL	5.2017 mL
	20 mM	0.1561 mL	0.7803 mL	1.5605 mL	3.9013 mL
	25 mM	0.1248 mL	0.6242 mL	1.2484 mL	3.1210 mL
	30 mM	0.1040 mL	0.5202 mL	1.0403 mL	2.6008 mL
	40 mM	0.0780 mL	0.3901 mL	0.7803 mL	1.9506 mL
	50 mM	0.0624 mL	0.3121 mL	0.6242 mL	1.5605 mL
	60 mM	0.0520 mL	0.2601 mL	0.5202 mL	1.3004 mL
	80 mM	0.0390 mL	0.1951 mL	0.3901 mL	0.9753 mL
	100 mM	0.0312 mL	0.1561 mL	0.3121 mL	0.7803 mL

PBD-150 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:

PBD-150790663-33-1PBD150PBD 150Amyloid-ββ-amyloid peptideAβAbetaAlzheimerInhibitorinhibitorinhibit

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PBD-150

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Complete Stock Solution Preparation Table

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